2. Apoptosis Cell Cycle/DNA Damage
  3. Apoptosis CDK
  4. CDK8-IN-13

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.

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CDK8-IN-13 Chemical Structure

CDK8-IN-13 Chemical Structure

CAS No. : 918523-75-8

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Based on 1 publication(s) in Google Scholar

CDK8-IN-13 Related Antibodies

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Description

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[1].

IC50 & Target[1]

CDK8

51.9 nM (IC50)

In Vitro

CDK8-IN-13 (compound 43; 1, 2.5, 5, 10 µM; 12 h) decreases the expression of p-STAT1 S727 and p-STAT5 S726 i a dose-dependent manner in HCT-116 cells[1].
CDK8-IN-13 (0, 1, 5, 10 µM; 48 h) induces apoptosis in a dose-dependent manner[1].

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

CDK8-IN-13 Related Antibodies

Cell Proliferation Assay[1]

Cell 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[1]

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, and suppressed the phosphorylation of STAT1 S727 induced by IFN-γ (10 ng/mL) in a dose-dependent manner.

Apoptosis Analysis[1]

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.
In Vivo

CDK8-IN-13 (40, 80 mg/kg; p.o.; for 15 days) inhibits tumor growth in a dose-dependent manner in mouse[1].
Pharmacokinetic Parameters of CDK8-IN-13 in Sprague-Dawley rats[1].

dose/routes t1/2 (h) Tmax (h) MRT(h)/td> Cmax (µg/L) AUC0-∞ (μg/L × h) CL (mL/h/kg) F (%)
10 mg/kg (po) 1.40 1.00 2.47 206.1 434.09 17.12 28.00
2 mg/kg (iv) 0.81 0.083 1.50 230.7 310.02 7.05 /
Sprague-Dawley rats, 2 mg/kg iv; 10 mg/kg po[1]

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

Animal Model: 6-week-old Balb/C mice (C1498 cells)[1]
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.
Molecular Weight

237.26

Formula

C14H11N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=CC(C2=CN=C3NC=CC3=C2)=C1)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (526.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2148 mL 21.0739 mL 42.1479 mL
5 mM 0.8430 mL 4.2148 mL 8.4296 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.2148 mL 21.0739 mL 42.1479 mL 105.3696 mL
5 mM 0.8430 mL 4.2148 mL 8.4296 mL 21.0739 mL
10 mM 0.4215 mL 2.1074 mL 4.2148 mL 10.5370 mL
15 mM 0.2810 mL 1.4049 mL 2.8099 mL 7.0246 mL
20 mM 0.2107 mL 1.0537 mL 2.1074 mL 5.2685 mL
25 mM 0.1686 mL 0.8430 mL 1.6859 mL 4.2148 mL
30 mM 0.1405 mL 0.7025 mL 1.4049 mL 3.5123 mL
40 mM 0.1054 mL 0.5268 mL 1.0537 mL 2.6342 mL
50 mM 0.0843 mL 0.4215 mL 0.8430 mL 2.1074 mL
60 mM 0.0702 mL 0.3512 mL 0.7025 mL 1.7562 mL
80 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3171 mL
100 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0537 mL
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CDK8-IN-13 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CDK8-IN-13918523-75-8ApoptosisCDKCyclin dependent kinaseHCT-116 cellsapoptosisorally activep-STAT1 S727p-STAT5 S726antitumorInhibitorinhibitorinhibit

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