About 13 results found for searched term "RA375" (0.207 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M5919 | Ramelteon (TAK-375) | Melatonin Receptor |
| TAK-375 | ||
| Ramelteon (TAK-375) is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively. | ||
| M40682 | RA375 | Proteasome |
| RA375 is an inhibitor of the 26S proteasome subunit RPN13. It can activate UPR signaling, generate ROS and activate apoptosis in cancer cells, and its anti-tumor activity is 10 times higher than that of RA190. | ||
| M4288 | Atractylenolide I | TLR |
| Atractylenolide I is a sesquiterpene obtained from the roots of Atractylenolide. Atractylenolide I has neuroprotective, anti-allergic, anti-inflammatory and anticancer activities. Atractylenolide I is an antagonist of TLR4 and can also reduce the phosphorylation of JAK2 and STAT3 in A375 cells. | ||
| M8758 | GW806742X | Necroptosis |
| GW806742X is an ATP site-targeing kinase inhibitor (IC50 in nM = 2/VEGFR2, 15/SRC, 47/C-FMS, 851/GSK3, 9016/ERBB2, 9120/FGFR) with potent antiproliferation activity against cancer cultures (IC50 in nM = 5/HUVEC-v, 424/HUVEC-b, 81/HEF, 453/MDA468, 470/A375P, 693/HT29, 734/PC3), GW806742X is now better known as Compound 1 for its anti-necroptosis activity via affinity interaction with ML | ||
| M9492 | B-Raf inhibitor 1 | Raf |
| ABM-0403 | ||
| B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 µM and 2 nM for A375 proliferation and A375 p-ERK, respectively. | ||
| M13642 | CX-5461 dihydrochloride | DNA/RNA Synthesis |
| CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM). | ||
| M14169 | GDC-0623 | MEK |
| RG 7421; MEK inhibitor 1 | ||
| GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM). | ||
| M14911 | CH6953755 | Src-bcr-Abl |
| CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo. | ||
| M16449 | Harringtonolide | FAK |
| Harringtonolide is a potent RACK1 inhibitor (IC50=39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction between FAK and RACK1. | ||
| M28109 | PF-3758309 hydrochloride | PAK |
| PF-03758309 hydrochloride | ||
| PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation. | ||
| M28529 | ML375 | AChR/AChE |
| VU0483253 | ||
| ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4. | ||
| M31007 | PF-3758309 dihydrochloride | PAK |
| PF-03758309 dihydrochloride | ||
| PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation. | ||
| M42974 | Benzyl DC-81 | Others |
| Benzyl DC-81 is an anticancer agent with antiproliferative activity against A375 and MCF-7 cells. | ||
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