MC180295

SKU: orb1225612

Description

MC180295 (MC-180295, MC 180295) is a novel potent, highly selective CDK9 inhibitor with IC50 of 5 nM, displays >22-fold selectivity over other CDKs; also shows high selectivity against a panel of 250 kinases at 1 uM; specificly inhibits the phosphorylation levels of Ser2 (pSer2); CDK9-mediated phosphorylation of BRG1 prevents it from being recruited to heterochromatin loci, while CDK9 inhibition allows BRG1 to remodel chromatin and alter gene expression; demonstrates broad anti-cancer activity in vitro and is effective in in vivo cancer models; also sensitize to anti-PD1 in vivo, increases the numbers of CD45+ immune cells and the percentages of CD3+ T cells and activates dendritic cells in the tumor environment, while not kill human T lymphocytes and did not affect the ratio of CD4 and CD8 T cells in vivo.

Key Properties

• CAS Number: 2237942-08-2
• MW: 358.416
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₈N₄O₃S
• SMILES: O=C(C1=C(N)N=C(N[C@@H]2C(C3)CCC3C2)S1)C4=CC=CC=C4[N+]([O-])=O
• Target: CDK
• Solubility: DMSO : 100 mg/mL 279.01 mM

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MC-180295 | MC 180295

Quick Database Links

Gene Symbol

CDK