Art. -Nr.: HY-149974

CDK8-IN-13

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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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Reinheit: 99.14%
CAS. Nr.: 918523-75-8
Formel: C₁₄H₁₁N₃O
Molecular Weight:237.26

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CDK8-IN-13 Chemical Structure

CAS. Nr.: 918523-75-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK8

51.9 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	GI₅₀	>50 μM Compound: 43	Antiproliferative activity against human A-375 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human A-375 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
A549	GI₅₀	>50 μM Compound: 43	Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
GES1	GI₅₀	>100 μM Compound: 43	Antiproliferative activity against human GES1 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human GES1 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
HCT-116	GI₅₀	>50 μM Compound: 43	Antiproliferative activity against human HCT-116 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
HL-60	GI₅₀	1 μM Compound: 43	Antiproliferative activity against human HL-60 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
HT-29	GI₅₀	>50 μM Compound: 43	Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MDA-MB-231	GI₅₀	>50 μM Compound: 43	Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MGC-803	GI₅₀	>50 μM Compound: 43	Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MOLM-13	GI₅₀	1.57 μM Compound: 43	Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MV4-11	GI₅₀	4.61 μM Compound: 43	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
SW480	GI₅₀	>50 μM Compound: 43	Antiproliferative activity against human SW480 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human SW480 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]

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.

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	t_1/2 (h)	T_max (h)	MRT(h)/td>	C_max (µg/L)	AUC_0-∞ (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.

Chemical Information

CAS. Nr. 918523-75-8
Appearance Solid
Molecular Weight 237.26
Formel C₁₄H₁₁N₃O
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.2148 mL

21.0739 mL

42.1479 mL

5 mM

0.8430 mL

4.2148 mL

8.4296 mL

10 mM

0.4215 mL

2.1074 mL

4.2148 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhang XX, et al. Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia. Eur J Med Chem. 2023 May 5;251:115214. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CDK8-IN-13

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CDK8-IN-13 Related Classifications

HY-149974 Related Classifications