MC180295  (Synonyms: (rel)-MC180295)

MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC₅₀ of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect^[1].

MC180295 is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC₅₀ of 5 nM, at least 22-fold more selective for CDK9 over other CDKs, such as CDK1-Cyclin B (IC₅₀, 138 nM), CDK2-Cyclin A (IC₅₀, 233 nM), CDK2-Cyclin E (IC₅₀, 367 nM), CDK3-Cyclin E (IC₅₀, 399 nM), CDK4-Cyclin D (IC₅₀, 112 nM), CDK5-P35 (IC₅₀, 159 nM), CDK5-P25 (IC₅₀, 186 nM), CDK6-Cyclin D3 (IC₅₀, 712 nM), and CDK7-CycH/MAT1 (IC₅₀, 555 nM). MC180295 also inhibits GSK-3α and GSK-3β^[1].
MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation^[1].
MC180295 (0.1 μM) inhibits the proliferation in cancer cells^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MC180295 (20 mg/kg, i.p., qod) inhibits significant anti-tumor activity in mice bearing SW48 cells, shows no inhibitory activity against human T cell growth in vivo^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

358.41

Solid

C₁₇H₁₈N₄O₃S

2237942-08-2

NC1=C(C(C2=CC=CC=C2[N+]([O-])=O)=O)SC(N[[email protected]@H]3[[email protected]](C4)CC[[email protected]]4C3)=N1

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

• [1]. Zhang H, et al. Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer. Cell. 2018 Nov 15;175(5):1244-1258.e26.  [Content Brief]