About 24 results found for searched term "WS-12" (0.124 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M20815 | WS-12 | TRP Channel |
| Acoltremon; AR-15512; AVX-012 | ||
| WS-12 (Acoltremon, AR-15512, AVX-012) is a potentially first-in-class, potent TRPM8 agonist with an EC50 of 39 nM. can be used in studies of dry eye and chronic neuropathic pain. | ||
| M6161 | GSK369796 Dihydrochloride | Potassium Channel |
| GSK369796 shows antimalerial activity with IC50 values of 11.2 nM for 3D7 strain, 12.6 nM for HB3 strain, 17.6 nM for K1 strain. | ||
| M10966 | SY-5609 | CDK |
| CDK7-IN-3 | ||
| SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a KD of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (Ki=2600 nM), CDK9 (Ki=960 nM), CDK12 (Ki=870 nM). | ||
| M14778 | Tafamidis meglumine | Transthyretin (TTR) |
| Fx-1006A | ||
| Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. | ||
| M20649 | LIT-927 | CXCR |
| LIT-927 is a novel neutraligand of CXCL12 with Ki value of 267 nM for inhibition of Texas red-labeled CXCL12 (CXCL12-TR) binding. It shows high selectivity toward CXCL12 vs other chemokines also involved in asthma. | ||
| M28066 | KNT-127 | Opioid Receptor |
| KNT-127 is a potent and selective δ-opioid receptor agonist effective by systemic administration. KNT-127 shows selectivity for the δ-receptor (Ki 0f 21.3, 0.16, 153 nM for opioid μ-, δ-, and κ-receptors, respectively). KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens and median pre-frontal cortex. | ||
| M28461 | AGI-12026 | Dehydrogenase |
| AGI-026 | ||
| AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma. | ||
| M28611 | Benzomalvin A | Neurokinin Receptor |
| Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively. | ||
| M28756 | JH-VIII-157-02 | ALK |
| JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells. | ||
| M28847 | MMP2-IN-2 | MMP |
| MMP2-IN-2 (compound 42) is a potent and selective MMP-2 (matrix metalloproteinases) inhibitor, with an IC50 of 4.2 μM. MMP2-IN-2 also shows inhibitory activity against MMP-13, MMP-9 and MMP-8, with IC50 values of 12, 23.3, and 25 μM, respectively. | ||
| M28992 | RapaLink-1 | mTOR |
| RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin with MLN0128 by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity. | ||
| M29370 | HG-12-6 | IRAK |
| HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation. | ||
| M29432 | WS-383 free base | E1/E2/E3 Enzyme |
| WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2. | ||
| M29433 | WS-383 | E1/E2/E3 Enzyme |
| WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2. | ||
| M29460 | SGC-iMLLT | Epigenetic Reader Domain |
| SGC-iMLLT is a first-in-class chemical probe and a potent, selective inhibitor of MLLT1/3-histone interactions with an IC50 of 0.26 μM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with Kds of 0.129 and 0.077 μM, respectively. | ||
| M29620 | PF-07038124 | PDE |
| PF-07038124 is a PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 shows inhibitory activities against IL-13, IL4, and IFNγ (IC50=125, 4.1 1.06 nM, respectively). | ||
| M29821 | HS-276 | IRAK |
| HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 can be used for rheumatoid arthritis (RA) research. | ||
| M30259 | (E)-Ferulic acid | Wnt/beta-catenin |
| (E)-Coniferic acid | ||
| (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299. | ||
| M30480 | Arotinolol | Adrenergic Receptor |
| Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases. | ||
| M30487 | ARM1 | Aminopeptidase |
| 4BSA | ||
| ARM1 (4BSA) is a potent aminopeptidase and epoxide hydrolase inhibitor. ARM1 shows aminopeptidase inhibitory activity with an IC50 7.61 µM and epoxide hydrolase inhibitory activity with an IC50 12.4 µM. | ||
| M30698 | AZ12253801 | IGF-1R |
| AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity. | ||
| M30731 | SLEC-11 | Others |
| SLEC-11 acts as a potential synthetic lethal lead for the research of gastric cancer. AL-GDa62 shows EC50 of 12.2 μM and 8.2 μM for isogenic mammary epithelial cells MCF10A-WT (wild-type) and MCF10A-CDH1-/-. | ||
| M30833 | Trifarotene | RAR/RXR |
| CD5789 | ||
| Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ∼65-fold and ∼16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM), respectively. | ||
| M38782 | Antimalarial agent 12 | Parasite |
| Antimalarial agent 12 is a potent antimalarial agent. Antimalarial agent 12 shows growth inhibition on P. falciparum Dd2 Strain (EC50=155 nM), 3D7 strain (EC50=136 nM). Antimalarial agent 12 has CC50 values of 10,000 to 50,000 nM for HEK-293 and hPHep cell lines. | ||
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