| New Inhibitors April 2016 |
| Proteasome Inhibitors |
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| Epoxomicin is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate. |
| Related Products: Bortezomib (PS-341), MG-132, Carfilzomib (PR-171) |
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| IAP Inhibitors |
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| AT406 (SM-406, ARRY-334543) is a potent Smac mimetic and an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1. |
| Related Products: Embelin, BV-6, Birinapant |
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| Bcr-Abl Inhibitors |
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| Radotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia. |
| Related Products: Imatinib Mesylate , Ponatinib, Nilotinib |
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| ROCK Inhibitors |
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| Ripasudil (K-115) is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension. |
| Related Products: Y-27632 2HCl, Fasudil, Thiazovivin |
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| Histone Methyltransferase Inhibitors |
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| SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 andKd of 31 nM and 53 nM, respectively. |
| Related Products: GSK343, BIX 01294, EPZ5676 |
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| Other New Compounds Available in April : |
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