CDK8-IN-9

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CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC₅₀ value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies.

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CDK8-IN-9 Chemical Structure

CAS No. : 2850253-95-9

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Biological Activity
Purity & Documentation
References
Customer Review

Description

CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC₅₀ value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
CT26	GI₅₀	4 μM Compound: 22	Antiproliferative activity against mouse CT26 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against mouse CT26 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 36068975]
GES1	GI₅₀	61.5 μM Compound: 22	Cytotoxicity against human GES1 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against human GES1 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 36068975]
HCT-116	GI₅₀	4.9 μM Compound: 22	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 36068975]
HT-29	GI₅₀	4.3 μM Compound: 22	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 36068975]
SW480	GI₅₀	2.1 μM Compound: 22	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 36068975]

In Vitro

CDK8-IN-9 (compound 22) (0-100 μM, 48 h) can significantly inhibit cell proliferation and target CDK8 to inhibit the activation of the WNT/β-catenin pathway, thereby suppressing β-catenin-mediated transcriptional activity of TCF/ LEF^[1].
CDK8-IN-9 (compound 22) (0.5,1 and 2 μM, 24 h) induces G2/M and S-phase cell cycle arrest, thereby inhibiting cell proliferation rather than inducing apoptosis^[1].

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

Cell Viability Assay^[1]

Cell Line:	HCT-116, HT-29, SW-480, CT-26 and GES-1 cells
Concentration:	0-100 μM
Incubation Time:	48 hours
Result:	Inhibited HCT-116, HT-29, SW-480, CT-26 and GES-1 cells with the GI₅₀ values of 4.9, 4.3, 2.1, 4.0 and 61.5 μM, respectively.

Cell Cycle Analysis^[1]

Cell Line:	HCT-116 cells
Concentration:	0.5, 1, and 2 μM
Incubation Time:	24 hours
Result:	Arrested cells in G2/M phase by 17%, 20.26% and 34.45% at concentrations of 0.5, 1, and 2 μM, respectively. Showed a decrease in the G0/G1 phase and a slight increase in the S phase.

In Vivo

CDK8-IN-9 (compound 22) (p.o., 20, 40 and 80 mg/kg, daily, 3 weeks) significantly reduces in tumor volume and inhibits weight loss in mice at the concentration of 80 mg/kg in Balb/c mice infected with CT-26 murine colon cancer cells^[1].

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

Animal Model:

Sprague−Dawley rats^[1]

Dosage:

10 mg/kg or 5 mg/kg

Administration:

p.o. for 10 mg/kg and i.v. for 5 mg/kg

Result:

The pharmacokinetic parameters of CDK8-IN-9 (compound 22)

Parameters	t_1/2 (h)	T_max (h)	MRT (h)	C_max (μg/L)	AUC_0-∞ (μg/L·h)	CL (L/h/kg)	F (%)
10 mg/kg (po)	1.21	0.75	2.022	497.56	783.66	9.23	39.8
5 mg/kg (iv)	1.63	-	1.756	706.29	983.09	11.32	-

Molecular Weight

423.43

Formula

C₂₄H₂₀F₃N₃O

CAS No.

2850253-95-9

SMILES

O=C(NC1=CC=C(C)C(C(F)(F)F)=C1)CCC2=CC=CC(C3=CN=C(NC=C4)C4=C3)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Xing Xing Zhang, et al. Discovery of the Novel 1H-Pyrrolo[2,3-b]pyridine Derivative as a Potent Type II CDK8 Inhibitor against Colorectal Cancer. J. Med. Chem.

CDK8-IN-9 Related Classifications

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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-92850253-95-9CDKCyclin dependent kinaseCDK8tumorcolorectal cancerInhibitorinhibitorinhibit

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