产品说明
生化/生理作用
LDC000067 (LDC067) is an ATP-competitive, potent and selective cyclin-dependent kinase 9 (CDK9) inhibitor (IC50 = 44 nM/CDK9-CycT1 vs. 5.51 μM/CDK1-CycB1, 2.44 μM/CDK2-CycA, 9.24 μM/CDK4-CycD1, >10 μM/CDK6-CycD3 & CDK7-CycH-MAT1; Kd = 32.7 nM/CDK9-CycT1 vs. 1.01 μM/CDK2-CycA, 16.0 μM/CDK7-CycH-MAT1) with much reduced or little potency against a panel of 28 non-CDK kinases. LDC067 selectively inhibits cellular RNA polymerase II CTD Ser2 phosphorylation (by 40% in HeLa; 60-min, 10 μM LDC067), but not CDK9-independent pSer5 or pSer7, causing apoptosis induction (by 239% and 200% of untreated control in A549 and MCF7 cultures) as a result of blocking RNAPII-mediated mRNA synthesis.
基本信息
| 经验(实验)分子式 | C18H18N4O3S · xHCl |
| 分子量 | 370.43 (free base basis) |
| MDL编号 | MFCD28137788 |
| NACRES | NA.77 |
产品性质
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 储存条件 | protect from light |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear (warmed) |
| 储存温度 | −20℃ |
| SMILES string | O=S(CC1=CC(NC2=NC=NC(C3=CC=CC=C3OC)=C2)=CC=C1)(N)=O |
安全信息
| 储存分类代码 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
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