2613307-67-6
2613307-67-6 structure
- Name: CDK8-IN-12
- Chemical Name: CDK8-IN-12
- CAS Number: 2613307-67-6
- Molecular Formula: C21H20ClN3O2
- Molecular Weight: 381.86
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2023-06-19 17:55:07
- Modify Date: 2024-03-09 06:31:22
-
CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent[1].
| Name | CDK8-IN-12 |
|---|
| Description | CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent[1]. |
|---|---|
| Related Catalog | |
| Target |
CDK8:14 nM (Ki) GSK-3α:13 nM (Ki) GSK-3β:4 nM (Ki) PKCθ:109 nM (Ki) |
| In Vitro | CDK8-IN-12 (化合物 38) 选择性抑制 MV4-11 急性髓性白血病细胞的增殖，GI50 为 0.36 μM[1]。 CDK8-IN-12 (0.36, 0.72 μM; 2 小时) 显着降低 STAT1 丝氨酸 727 的磷酸化[1]。 Western Blot Analysis[1] Cell Line: MV4-11 cells Concentration: 0.36, 0.72 μM Incubation Time: 2 hours Result: Significantly reduced the phosphorylation of serine 727 on STAT1 at concentrations of their respective 1× GI50 values, but barely affected the level of total STAT1. |
| In Vivo | CDK8-IN-12 (化合物 38; 静脉给药; 大鼠 5 mg/kg; 小鼠 2 mg/kg) 对大鼠和小鼠的 T1/2 分别为 0.9 小时和 0.34 小时[1]。 |
| References |
| Molecular Formula | C21H20ClN3O2 |
|---|---|
| Molecular Weight | 381.86 |