CDK8-IN-13

Research use only, not for human use.

CDK8-IN-13 is a CDK8 inhibitor (IC50: 51.9 nM) with potent, selective and oral activity. CDK8-IN-13 induces apoptosis and reduces the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 exhibits anti-tumour activity.

CDK8-IN-13 is a potent, selective and orally active CDK8 inhibitor with an IC50 value of 51.9 nM. CDK8-IN-13 induces Apoptosis. CDK8-IN-13 decreases the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 shows antitumor activity.

Cell Proliferation AssayCell Line:molm-13, HL-60, MV4-11, MGC-803, MDA-MB-231, A375, A549 cells Concentration:0-50 μM Incubation Time:Result:Showed antiproliferative activity with GC50s of 1.57, 1.00, 4.61, >50, >50, >50, >50 μM, respectively.Western Blot Analysis Cell Line:HCT-116 cells Concentration:1, 2.5, 5, 10 μM Incubation Time:12 h Result:Decreased the expression of p-STAT1 S727 and p-STAT5 S726, andsuppressed the phosphorylation of STAT1 S727 induced by IFN-γ (10 ng/mL) in a dose-dependent manner.Apoptosis Analysis Cell Line:HL-60 cells Concentration:0, 1, 5, 10 μM Incubation Time:48 h Result:Induced approximately 7% and 36% apoptotic at concentrations of 5 and 10 μM, respectively.

Animal Model:6-week-old Balb/C mice (C1498 cells)Dosage:40, 80 mg/kg Administration:P.o.; for 15 days Result:Decreased the tumor growth with no significant weight loss,the expression of Ki67 decreased in a dose-dependent manner, the level of phosphorylation of STAT1 S727 in tumor tissues was downregulated.

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Apoptosis

Apoptosis

Apoptosis | CDK

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918523-75-8

237.26

C14H11N3O

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (526.85 mM; Ultrasonic )

C(N)(=O)C=1C=C(C=2C=C3C(=NC2)NC=C3)C=CC1

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(-20℃)

With Ice Pack

≥ 2 years