E1611 |
Atuzabrutinib |
|
Jul 25 2024 |
E1791 |
Zongertinib |
|
Jul 25 2024 |
E1931 |
AD-5584 |
|
Jul 25 2024 |
E1533 |
Lipofermata |
|
Jul 25 2024 |
E1877 |
BLU 451(LNG-451) |
|
Jul 24 2024 |
E4827 |
Diphenhydramine |
|
Jul 23 2024 |
E1889 |
PCO371 |
|
Jul 23 2024 |
E1985 |
YD23 |
|
Jul 23 2024 |
E4835 |
Sumatriptan |
|
Jul 23 2024 |
E4836 |
Bupivacaine |
|
Jul 23 2024 |
E1961 |
NVL-655 |
|
Jul 23 2024 |
E1015 |
Angiotensin II human |
|
Jul 23 2024 |
E4837 |
Trimethoprim (lactate) |
|
Jul 23 2024 |
E4647 |
Aticaprant |
|
Jul 23 2024 |
E1957 |
NX-1607 |
|
Jul 23 2024 |
E4826 |
L-Ornithine L-aspartate |
L-ornithine-L-aspartate (LOLA) is a stable salt composed of two natural nonessential L-amino acids: ornithine and aspartic acid. It effectively lowers blood ammonia concentration by enhancing ammonia detoxification in the muscles, and alleviating hepatic encephalopathy symptoms in liver cirrhosis. |
Jul 19 2024 |
E4822 |
Tacrine |
Tacrine is a potent acetylcholinesterase (AChE) inhibitor. It inhibits acetylcholinesterase(AChE) and butyrylcholinesterase(BChE) with an IC50 of 77 nM and 69 nM, respectively. It is used in the treatment of Alzheimer's disease (AD), also poisoning topoisomerases and inhibiting in vivo (mitochondrial)mtDNA synthesis. |
Jul 19 2024 |
E4832 |
DL-Alanine |
DL-alanine (DL-2-Aminopropionic acid) is a racemic mixture of L- and D-alanine that forms complexes with transition metals like Cu(II), Zn(II), and Cd(II). It also plays a key role in the glucose-alanine cycle between tissues and the liver. |
Jul 19 2024 |
E4831 |
L-Arginine (L-glutamate) |
L-Arginine (L-glutamate) (Arginine glutamate) is a mixture of amino acids that induces apoptosis via hypertonic stress. It also promotes gastric relaxation by providing L-arginine for nitric oxide production, thereby benefiting gastrointestinal motility and conditions associated with vagus nerve dysfunction. |
Jul 19 2024 |
E4830 |
Guanidine thiocyanate |
Guanidine thiocyanate is a potent inhibitor of nucleases and a powerful denaturant of proteins. It is used for RNA isolation due to its strong chaotropic properties, which effectively denature RNase enzymes in samples, ensuring RNA stability and purity during extraction processes. Nucleic acid extraction buffers containing guanidine thiocyanate effectively deactivate high-titer polioviruses found in potentially infectious materials. |
Jul 19 2024 |
E4825 |
Naphazoline (nitrate) |
Naphazoline (nitrate) is a agonist of peripheral α2-adrenergic receptor and used as a topical decongestant. It also acts as a vasoconstrictor that effectively reduces intraoperative bleeding and enhances postoperative analgesia. When used in conjunction with intranasal lidocaine, it significantly reduces both intra- and postoperative pain, thereby decreasing the need for rescue analgesics in the postoperative period following septorhinoplasty. |
Jul 19 2024 |
E4828 |
Cloperastine fendizoate |
Cloperastine fendizoate (Hustazol) is a sedative used to relieve cough and also has a peripheral action that desensitizes the afferent nerves in the tracheobronchial region. It inhibits the hERG K+ currents in a concentration-dependent manner, with an IC50 value of 0.027 μM. |
Jul 19 2024 |
E4824 |
Hydroxychloroquine |
Hydroxychloroquine (HCQ) is an antimalarial drug that inhibits autophagy and is used to treat systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA). It exhibits immunomodulatory, antithrombotic, and antiplatelet properties. It inhibits the release endothelin-1, a potent vasoconstrictor, and restores impaired angiogenesis in TNF-α-treated endothelial cells in vitro. It also reduces the production of inflammatory cytokines such as TNF-α, IFN-γ, and IL-6 from peripheral blood mononuclear cells, upregulates IL-10 and decreases platelet aggregation. |
Jul 19 2024 |
E4806 |
Quinine dihydrochloride |
Quinine dihydrochloride is an antiparasitic used to treat malaria and is particularly important for managing malaria during the first trimester of pregnancy. It inhibits Slo3 (KCa 5.1) channel, which are a significant part of the mammalian KSper (sperm potassium conductance), by binding to hydrophobic side chains located at the intracellular region of the channel pore. |
Jul 19 2024 |
E1885 |
LY3522348 |
LY3522348 is a highly selective oral dual inhibitor of the human ketohexokinase isoforms C and A, with IC50 values of 20nM for hKHK-C and 24nM for hKHK-A. It shows a significant pharmacodynamic effect in a mouse model of fructose metabolism. |
Jul 19 2024 |
E1686 |
SW-100 |
SW-100 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 2.3 nM. It displays 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. |
Jul 18 2024 |
E4630 |
Ilginatinib hydrochloride |
Ilginatinib hydrochloride (NS-018 hydrochloride) is a potent small-molecule inhibitor of JAK2 that is competitive with adenosine triphosphate (ATP) which exhibits 30–50-fold greater selectivity for JAK2 over other Jak-family kinases such as JAK1, JAK3, and TYK2.It inhibits JAK2, JAK1, JAK3, and TYK2 with IC50 of 0.72 nM, 33 nM, 39 nM, and 22 nM, respectively. It also showed potent inhibition of Src-family kinases, SRC and FYN. It can be used in research of myeloproliferative neoplasms. |
Jul 18 2024 |
E4823 |
Pargyline |
Pargyline is an irreversible selective inhibitor of monoamine oxidase (MAO) with Kis of 13 μM and 0.5 μM for MAO-A and MAO-B respectively. It has pharmaceutical potential as an anticancer drug for human prostate cancer. |
Jul 18 2024 |
E4829 |
Bismuth subnitrate |
Bismuth subnitrate is an antigastric ulcer and antidiarrheic agent that induces metallothionein (MT). It can be used as an adjunct in cancer chemotherapy to induce MT in target organs. |
Jul 18 2024 |
P1241 |
Bromelain |
Bromelain is an aqueous extract of pineapple that is composed of 95%-mixture of proteases, acting as an inhibitor of Prostaglandin E2 (PGE2) and Cox-2. It exhibits potent anti-inflammatory, anti-thrombotic, fibrinolytic and anti-cancer functions. |
Jul 18 2024 |
E4592 |
UGT8-IN-1 |
UGT8-IN-1 is a brain-penetrable and orally active inhibitor of ceramide galactosyltransferase enzyme (UGT8). UGT8-IN-1 targets sulfatide metabolism resulting in ceramide-induced lethal mitophagy and subsequent cancer cell death in vitro, and reduces tumour growth in mutant Kras; Gnas allografts. |
Jul 16 2024 |
E1966 |
VVD-214 |
VVD-214 (RO7589831, VVD-133214) is a synthetic allosteric inhibitor of WRN helicase. VVD-214 binds irreversibly to cysteine 727 on WRN, suppressing ATP hydrolysis and helicase activity. VVD-214 exhibits potent efficacy in inducing double-stranded DNA breaks, nuclear enlargement, and cellular apoptosis in cancers with high microsatellite instability (MSI). |
Jul 15 2024 |
E1970 |
BAL-0028 |
BAL-0028 (Compound 3), which belongs to the indazole class is an inhibitor of NLRP3 activation with an IC50 value of 25 nM. BAL-0028 binds tightly to the NACHT domain of NLRP3, with KD values ranging from 104 to 123 nM. BAL-0028 also exhibits anti-inflammatory activity. |
Jul 15 2024 |
E1186 |
Tenapanor |
Tenapanor (AZD1722, RDX5791) is a potent and orally active inhibitor of sodium/hydrogen exchanger isoform 3 (NHE3). It exhibits an IC50 of 2 and 6 nM in human and mouse ileum monolayers, respectively. Tenapanor reduces intestinal phosphate absorption predominantly by reducing passive paracellular phosphate flux. |
Jul 15 2024 |
E4821 |
Simvastatin acid (ammonium) |
Simvastatin acid (Tenivastatin) ammonium is a potent inhibitor of HMG-CoA reductase (HMGCR). Simvastatin acid ammonium also decreases Indoxyl sulfate-induced reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium regulates the expression of OATP3A1 in cardiomyocytes. |
Jul 15 2024 |
E4820 |
Sulbactam pivoxil |
Sulbactam pivoxil (CP 47904), a proagent of sulbactam, is an inhibitor of β-lactamase. Sulbactam pivoxil provides higher absorption than its parent compound and achieves high serum levels following oral administration. |
Jul 15 2024 |
E4818 |
Pemetrexed (disodium heptahydrate) |
Pemetrexed (disodium heptahydrate) is a folate antimetabolite that inhibits thymidylate synthase, dihydrofolate reductase and glycinamide ribonucleotide formyltransferase. It also induces apoptosis and cell-cycle arrest in non-small-cell lung cancer carrying an EGFR exon 19 deletion. |
Jul 14 2024 |
E1290 |
Ziftomenib |
Ziftomenib (KO-539) is an oral inhibitor of menin targeting the menin–KMT2A protein-protein interaction. It exhibits antileukemic activity and induces apoptosis of acute myeloid leukemia(AML) cells. |
Jul 11 2024 |
E4819 |
Afatinib free base |
Afatinib free base (Gilotrif, BIBW2992, Boehringer Ingelheim) is a second-generation tyrosine kinase inhibitor (TKI) that irreversibly inhibits EGFR and HER2, with IC50 of 0.5 nM, 0.4 nM, 14 nM and 1 nM for wild-type EGFR, EGFR-L858R, HER2, ErbB4, respectively. |
Jul 11 2024 |
E1867 |
NPD4928 |
NPD4928 is an inhibitor of Ferroptosis Suppressor Protein 1 (FSP1) that enhances ferroptosis. It enhances the cytotoxic effects on various cell types when combined with GPX4 antagonists. |
Jul 11 2024 |
E4816 |
Choline hydroxide, 42.5 wt.% in water |
Choline hydroxide, 42.5 wt.% in water (Sincaline), is a strong organic base used as a metal-free, nontoxic, and water-soluble catalyst. It facilitates the synthesis of 1,8-naphthyridine derivatives while avoiding the use of hazardous or carcinogenic organic solvents. |
Jul 10 2024 |
E1975 |
HC-7366 |
HC-7366, is a First-in-Human modulator of General controlled nonderepressible 2 (GCN2) that activates GCN2. It demonstrates anti-metastatic efficacy, reducing lung metastases and exhibits anti-tumor activity. |
Jul 09 2024 |
A2163 |
Anti-mouse IL-12 p40-InVivo |
Anti-mouse IL-12 p40-InVivo reacts with mouse p40 also known as IL-12β. p40 is a 40 kDa subunit of IL-12 and IL-23. IL-12 is a heterodimeric cytokine composed of subunits IL-12α p35 and IL-12β p40. |
Jul 09 2024 |
A2164 |
Anti-mouse B220-InVivo |
Anti-mouse B220-InVivo reacts with mouse B220 also known as CD45R. B220 is a 220 kDa transmembrane protein tyrosine phosphatase expressed on B cells and some subsets of T and NK cells. |
Jul 09 2024 |
E4805 |
Methylene Blue trihydrate |
Methylene blue trihydrate (C.I. Basic Blue 9 trihydrate) acts as an inhibitor of soluble guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS). Methylene blue trihydrate exhibits antimalarial, antidepressant, and anxiolytic activity effects. Methylene Blue trihydrate has potential applications in treating methemoglobinemia, neurodegenerative disorders, and ifosfamide-induced encephalopathy. |
Jul 08 2024 |
E4807 |
Dexketoprofen trometamol |
Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective inhibitor of COX. Dexketoprofen trometamol exhibits analgesic efficacy and can be used in treating acute pain. |
Jul 08 2024 |
E4811 |
Levofloxacin hydrochloride |
Levofloxacin hydrochloride ((-)-Ofloxacin hydrochloride), a synthetic fluoroquinolone antibiotic, is an inhibitor of DNA gyrase and Topoisomerase IV. It exhibits bactericidal effects by preventing bacterial DNA replication. |
Jul 08 2024 |
E4812 |
Fluoxetine |
Fluoxetine (LY-110140 free base) is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor. Fluoxetine is used widely in the treatment of depression, anxiety-related symptoms and also displays anticonvulsant activity. |
Jul 08 2024 |
E1987 |
APX2009 |
APX2009 is a second-generation redox-specific inhibitor of APE1/Ref-1, an essential enzyme in the base excision repair (BER) pathway. APX2009 effectively reduces breast cancer cell proliferation and colony formation. |
Jul 08 2024 |
E1944 |
INS018-055(ISM001-055) |
INS018-055 (ISM001-055, TNIK&MAP4K4-IN-2, compound 112) is an inhibitor of TNIK and MAP4K4. It exhibits an IC50 values of 12-120 nM on TNIK. |
Jul 08 2024 |
E1854 |
INX-315 |
INX-315 is an orally active and selective inhibitor of CDK2 that induces cell cycle arrest in the G1 phase. It exhibits an IC50 value of 2.3 nM in intracellular NanoBRET assay, respectively. It displays a 50-fold increased CDK2 selectivity compared to CDK1. INX-315 decreases the phosphorylation of CDK2 substrates and suppresses tumor growth in xenograft mouse models in a dose-dependent manner. |
Jul 05 2024 |
E1900 |
Simnotrelvir |
Simnotrelvir(SIM0417; SARS-CoV-2-IN-41) is an inhibitor of coronavirus main proteinase (3CLpro) (SARS-CoV-2 3CLpro) with an IC50 of 24 nM. It has a potential anti-SARS-CoV-2 activity. |
Jul 04 2024 |
E4809 |
Piperaquine tetraphosphate tetrahydrate |
Piperaquine tetraphosphate tetrahydrate is an inhibitor of autophagy . It is a bisquinoline antimalarial agent effective against Plasmodium falciparum. Piperaquine tetraphosphate tetrahydrate is useful in antimalarial research. |
Jul 04 2024 |
E4808 |
Propionyl-L-carnitine hydrochloride |
Propionyl-L-carnitine hydrochloride(Levocarnitine propionate hydrochloride) supports mitochondrial metabolism, offers cardiovascular benefits, acts as a free radical scavenger, and is used in treating colonic inflammatory bowel disease. |
Jul 04 2024 |
E4810 |
Piperacillin |
Piperacillin is a broad-spectrum β-lactam antibiotic with potent bactericidal activity against Gram-negative bacteria and selects Gram-positive strains via penicillin-binding proteins. |
Jul 04 2024 |
E4634 |
MIRA-1 |
MIRA-1(NSC 19630), a maleimide compound, is a selective inhibitor of Werner syndrome WRN helicase activity with an IC50 of 20 µM while sparing ATPase and exonuclease activities. It reactivates mutant p53, inducing apoptosis in various human solid tumor cell lines with tetracycline-regulated mutant p53. |
Jul 03 2024 |
E4803 |
Vardenafil |
Vardenafil is an orally active and selective inhibitor of phosphodiesterase-5 (PDE5), with an IC50 value of 0.7 nM, respectively. Vardenafil acts as a competitive inhibitor of cyclic guanosine monophosphate (cGMP) hydrolysis, thereby increasing cGMP levels. Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes. |
Jul 02 2024 |
E1848 |
BGB-8035 |
BGB-8035 is an orally active, highly selective inhibitor of Bruton's tyrosine kinase (BTK) with IC50 values of 1.1 nM for BTK, respectively. BGB-8035 exhibits antitumor and anti-arthritis activity and displays potential for its use in research of B-cell malignancies and autoimmune diseases. |
Jul 02 2024 |
E1558 |
GSK-3008348 HCl |
GSK-3008348 HCl is a small molecule antagonist of integrin αvβ6 with an affinity (pIC50) value of 8.1 for αvβ6 in cell Adhesion assays. |
Jul 02 2024 |
E1582 |
Edralbrutinib |
Edralbrutinib (TG-1701) is an irreversible, highly specific, and potent inhibitor of Bruton's tyrosine kinase (BTK). TG-1701 shows similar efficacy but greater selectivity compared to the first-in-class BTK inhibitor ibrutinib, with a Kd value of 3 nmol/L, in both in vitro and in vivo models of B-cell non-Hodgkin lymphoma (B-NHL). |
Jul 02 2024 |
E4804 |
Sitagliptin phosphate |
Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of dipeptidyl peptidase IV (DPP-4) with an IC50 value of 19 nM in Caco-2 cell extracts. |
Jul 02 2024 |
E4801 |
Cu(II)-Elesclomol |
Cu(II)-Elesclomol, a Cu2+ complex of Elesclomol, is a weak inhibitor of DNA topoisomerase I. It is also highly capable of inducing cuproptosis and apoptosis. It induces DNA double-strand breaks in K562 cells and causes a G1 cell cycle block. Cu(II)-Elesclomol displays anticancer activity. |
Jun 27 2024 |
E4802 |
Ticarcillin disodium |
Ticarcillin disodium is a semisynthetic β-lactam antibiotic, which is active against Pseudomonas aeruginosa, Escherichia coli, Pseudomonas mirabilis, Pseudomonas rettgeri, and Klebsiella aerogenes. |
Jun 27 2024 |
E1858 |
RMC-7977 |
RMC-7977 is a potent, reversible, tri-complex oral inhibitor that selectively targets active (GTP-bound) forms of KRAS, HRAS, and NRAS, which exhibits broad-spectrum activity against both mutant and wild-type variants (a RASMULTI (ON) inhibitor). It also exhibits significant anti-tumor efficacy in pancreatic ductal adenocarcinoma (PDAC). |
Jun 27 2024 |
E1857 |
TH-Z816 |
TH-Z816 is an inhibitor of ,KRAS(G12D) with an IC50 of 14 μM in an SOS-catalyzed nucleotide exchange assay with GDP as the incoming nucleotide. |
Jun 27 2024 |
E1865 |
Envonalkib |
Envonalkib(TQ-B3139; CT-71; Formula 1) is a potent and orally active inhibitor of ALK, that exhibits IC50 values of 1.96 nM, 35.1 nM, and 61.3 nM for wild-type and mutated L1196M and G1269S-ALK. Envonalkib is also used in the research of non-small cell lung cancer. |
Jun 27 2024 |
E1995 |
AZD-5462 |
AZD-5462(Example 1) is a modulator of RXFP1, the cognate receptor for human relaxin, that belongs to the GPCR family 1c number. AZD-5462 exhibits anti-fibrotic and anti-inflammatory properties. |
Jun 27 2024 |
E1824 |
Vazegepant hydrochloride |
Vazegepant hydrochloride (BHV-3500, Zavegepant), is a highly potent, selective, and structurally unique small molecule antagonist of CGRP receptor. It can also be used for the acute treatment of migraine. |
Jun 27 2024 |
E1703 |
SF2312 |
SF2312 is a highly potent inhibitor of Enolase with IC50s of 37.9 nM and 42.5 nM for human recombinant ENO1 and ENO2, respectively, and also is a natural phosphonate antibiotic. SF2312 displays activity against bacteria under anaerobic conditions. |
Jun 27 2024 |
E1932 |
DW71177 |
DW71177 is a potent BD1-Selective inhibitor of BET. DW71177 selectively interacts with BD1 and exhibits strong antileukemic activity. DW71177 can also be used in the study of acute myeloid leukemia. |
Jun 27 2024 |
E1846 |
TL13-112 |
TL13-112 is a degrader of anaplastic lymphoma kinase (ALK) with an IC50 of 0.60 nM. It demonstrates anti-proliferative activity in non-small-cell lung cancer (NSCLC) and anaplastic large cell lymphoma (ALCL) cell lines. |
Jun 25 2024 |
E1580 |
TNG260 |
TNG260 is an inhibitor of CoREST-selective deacetylase (CoreDAC) that inhibits HDAC1 with 10-fold selectivity over HDAC3. It decreases intratumoral neutrophil infiltration and exhibits immune-mediated cell killing. |
Jun 24 2024 |
E1188 |
Brensocatib |
Brensocatib (AZD7986, INS1007) is an oral, selective, reversible inhibitor of dipeptidyl peptidase-1 (DPP-1). It reduces the activity of all major neutrophil serine proteases (NSPs) including, neutrophil elastase (NE), proteinase 3 (PR3), and cathepsin G (CatG) in patients with bronchiectasis. |
Jun 24 2024 |
P1238 |
SN 52 |
SN52, a cell-permeable peptide containing the p50 NLS, is a selective inhibitor of NF-κB pathway. It selectively and completely blocks the ionizing radiation (IR)-induced nuclear import of p52 and RelB. It also enhances the radiosensitivity of prostate cancer cells. |
Jun 24 2024 |
E1660 |
NX-5948 |
NX-5948(BTK-IN-24) is a novel oral small molecule that induces BTK degradation via cereblon E3 ubiquitin ligase recruitment. It mediates potent anti-inflammatory activity and can cross the blood-brain barrier in animal models. |
Jun 23 2024 |
E1986 |
TR-107 |
TR-107 is a chemical activator of the human mitochondrial protease ClpP with an EC50 of 140 nM. It exhibits excellent potency and specificity in the research of triple-negative breast cancer (TNBC) cell models. |
Jun 23 2024 |
E1947 |
DiR (Cy7 DiC18) |
DiR (Cy7 DiC18) is a near-infrared fluorescent long-chain carbocyanine dye used for labeling cell membranes, organelles, liposomes, viruses, and lipoproteins in vivo and in vitro. |
Jun 23 2024 |
E1437 |
PHI-101 |
PHI-101 is an orally active, potent third-generation inhibitor of FLT3 that overcomes resistance to multiple drug-resistant mutations. It has potential for research in relapsed or refractory acute myeloid leukemia (AML). |
Jun 23 2024 |
E1751 |
MSC-4381 |
MSC-4381 (MCT4-IN-1) is an orally active, selective inhibitor of monocarboxylate transporter 4 (MCT4) with an IC50 of 77 nM and a Ki of 11 nM. It has the potential to inhibit lactate efflux and promote intracellular lactate accumulation in MCT4-expressing cell lines. |
Jun 23 2024 |
E4607 |
Oseltamivir acid |
Oseltamivir acid(GS 4071;Ro 64-0802;Oseltamivir carboxylate), a metabolite of the antiviral compound oseltamivir, acts as a competitive inhibitor of influenza neuraminidases A and influenza neuraminidases B with IC50 of 0.1 to 4.9 nM respectively, thereby preventing virus budding and release. |
Jun 23 2024 |
E4594 |
Lithium iodide hydrate |
Lithium iodide hydrate is a reagent and the water-crystallized form of lithium iodide. It is commonly used as an electrolyte additive in dye-sensitized solar cells and Li-S batteries, enhancing their cycle life. |
Jun 23 2024 |
E4606 |
Dihexa |
Dihexa(PNB-0408), an oligopeptide drug, is an orally active and blood-brain barrier-permeable analog of angiotensin IV. It binds to hepatocyte growth factor (HGF) with high affinity and potentiates its activity at its receptor, c-Met. Dihexa can also be used as a therapeutic potential in the treatment of Alzheimer’s disease. |
Jun 19 2024 |
E1917 |
SLF1081851 hydrochloride |
SLF1081851 hydrochloride is a potential inhibitor of Spns2 that blocks S1P release with an IC50 of 1.93 μM. It can be developed as a probe for studying Spns2 biology and immune modulation. |
Jun 18 2024 |
E1528 |
RP-6685 |
RP-6685 is a potent, selective, and orally active inhibitor of DNA polymerase theta (Polθ). RP-6685 exhibits antitumor efficacy in animal models. |
Jun 18 2024 |
E1912 |
B102(PARP/HDAC-IN-1) |
B102(PARP/HDAC-IN-1) is a dual inhibitor of PARP and HDAC, with IC50 of 19.01 nM, 2.13 nM, 1.69 μM, > 10 μM for PARP1, PARP2, HDAC1, HDAC6, respectively, in an enzymatic assay. It exhibits anti-proliferative and anti-tumor effects. It also induces DNA damage and apoptosis in vitro. |
Jun 17 2024 |
E1980 |
Atogepant |
Atogepant(MK-8031, AGN-241689) is a potent, selective, orally available antagonist of the calcitonin gene-related peptide (CGRP) receptor, with ki of 0.026 nM for human CGRP receptor. It is used for the preventive treatment episodic migraine. |
Jun 17 2024 |
E1788 |
CQ211 |
CQ211 is a cell penetrant, potent and selective inhibitor of RIOK2(Right open reading frame kinase 2) with a Kd of 6.1 nM. It effectively inhibits cancer cell proliferation and shows promising in vivo efficacy in mouse xenograft models. |
Jun 13 2024 |
E1894 |
PROTAC tubulin-Degrader-1(compound W13) |
PROTAC tubulin-Degrader-1(compound W13) is an inhibitor of PROTAC tubulin exhibiting antitumor activity against human lung cancer. |
Jun 11 2024 |
P1239 |
ADH-1 |
ADH-1, an antagonist of N-cadherin, blocks N-cadherin-mediated cell adhesion. It exhibits significant antitumor activity against N-cadherin-expressing cells in vitro assays. |
Jun 10 2024 |
E1949 |
DuP-697 |
DuP-697 is a potent, irreversible, selective, and orally active inhibitor of COX-2 with an IC50 value of 10 nM for human COX-2, respectively. DuP-697 exerts antiproliferative, antiangiogenic, and apoptotic effects in colorectal cancer cells. |
Jun 10 2024 |
E1662 |
Elenestinib phosphate |
Elenestinib phosphate(BLU-263 phosphate) is a potent and orally active inhibitor of tyrosine kinase that exhibits potent inhibition of c-KIT (D816V) mutation. BLU-263 phosphate has the potential for its use in the research of systemic mastocytosis (SM). |
Jun 10 2024 |
E1908 |
HRO761 |
HRO761 is a potent, selective, allosteric inhibitor of Werner syndrome RecQ helicase (WRN). It binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation, and demonstrates anti-proliferative effects specifically in microsatellite instability (MSI) cancer cells. |
Jun 10 2024 |
E4596 |
GSK-2879552 |
GSK-2879552 is a selective and potent inhibitor of Lysine-specific demethylase 1 (LSD1, KDM1A), with the potential to treat Small cell lung cancer (SCLC). It induces the expression of putative KDM1A target genes and demonstrates potent, predominantly cytostatic, antiproliferative activity in SCLC cell lines and tumor xenograft models. |
Jun 07 2024 |
E4595 |
SB-743921 |
SB-743921 (SB-921) is an inhibitor of Kinesin Spindle Protein (KSP), a mitotic protein essential for cell cycle control and motility. It functions by selectively targeting rapidly dividing cells and disrupting spindle formation during cell division, leading to G2/M phase arrest and ultimately causing cell death. It also inhibits proliferation and induces apoptosis in diffuse large B-cell lymphoma (DLBCL) cell lines. |
Jun 07 2024 |
S7512 |
GSK269962A |
GSK269962A is a potent and selective inhibitor of ROCK with IC50 values of 1.6 nM for ROCK1 and 4 nM for ROCK2. It shows potential as an alternative treatment for overactive bladder (OAB), and also exhibits anti-inflammatory and vasodilatory activities. |
Jun 06 2024 |
S9894 |
Vafidemstat |
Vafidemstat(ORY-2001) is a potent, selective, brain-penetrant dual inhibitor of lysine-specific histone demethylase (LSD1, KDM1A) and MAO-B, with IC50 values of 105 nM and 58 nM, respectively. It shows potential for treating memory deficits and behavioral alterations in neurodegenerative and psychiatric diseases. |
Jun 06 2024 |
E4593 |
Benzo-15-crown-5 ether |
Benzo-15-crown-5-ether (B15C5) is employed as a ligand in metal-catalyzed reactions to improve reactivity and selectivity by coordinating with metal cations. Additionally, it serves as a chelating agent for sodium and potassium ions. |
Jun 06 2024 |
E1872 |
Selnoflast |
Selnoflast(RO-7486967) is a selective and reversible small molecule inhibitor of NLRP3 inflammasome, with the potential to treat moderate to severe active ulcerative colitis. |
Jun 03 2024 |
E1625 |
Elsubrutinib |
Elsubrutinib(ABBV-105) is a covalent, irreversible, potent, and highly selective inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 0.18 μM for BTK catalytic domain. It specifically inhibits BTK dependent cellular functions, including both BCR and FcγR mediated signaling. It also exhibits significant efficacy in pre-clinical mechanistic models of antibody production, as well as in models of rheumatoid arthritis and lupus. |
Jun 03 2024 |