1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK8/19-IN-1

CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.

For research use only. We do not sell to patients.

CDK8/19-IN-1 Chemical Structure

CDK8/19-IN-1 Chemical Structure

CAS No. : 1818427-07-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 881 In-stock
Solution
10 mM * 1 mL in DMSO USD 881 In-stock
Solid
1 mg USD 404 In-stock
5 mg USD 930 In-stock
10 mg USD 1300 In-stock
25 mg USD 2210 In-stock
50 mg USD 3090 In-stock
100 mg USD 4325 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.

IC50 & Target[1]

CDK8/CycC

0.46 nM (IC50)

CDK19/CycC

0.99 nM (IC50)

CDK9

270 nM (IC50)

In Vitro

CDK8/19-IN-1 (52h) is a potent CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively. CDK8/19-IN-1 also weakly inhibits CDK2, with 62% inhibition at 1 μM. CDK8/19-IN-1 (1 μM) shows >50% inhibition against GSK3β, PLK1, ASK1, CK1δ, PKA, ROCK1, PKCθ, CDC7. CDK8/19-IN-1 shows Kds of 25, 46, 81, 86, 97, 160 and >3000 nM for CDK19, CDK8, DYRK1B, HASPIN, YSK4, HIPK1 and EPHA3, respectively. CDK8/19-IN-1 displays potent antitumor activity, with GI50 of 0.43-2.5 nM for colon, multiple myeloma, acute myelogenous leukemia (AML), lung cancer cells[1].

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

In Vivo

CDK8/19-IN-1 (52h; 1.25 mg/kg twice daily or 2.5 mg/kg once daily, p.o.) significantly suppresses tumor growth in mice bearing RPMI8226 human hematopoietic and lymphoid cells[1].

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

Molecular Weight

430.50

Formula

C19H18N4O4S2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=C2CCC3=C(SN=C3)C2=C(OC4=CC=C(C(NCCOC)=O)N=C4)S1)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 : 50 mg/mL (116.14 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 2.3229 mL 11.6144 mL 23.2288 mL
5 mM 0.4646 mL 2.3229 mL 4.6458 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 2.3229 mL 11.6144 mL 23.2288 mL 58.0720 mL
5 mM 0.4646 mL 2.3229 mL 4.6458 mL 11.6144 mL
10 mM 0.2323 mL 1.1614 mL 2.3229 mL 5.8072 mL
15 mM 0.1549 mL 0.7743 mL 1.5486 mL 3.8715 mL
20 mM 0.1161 mL 0.5807 mL 1.1614 mL 2.9036 mL
25 mM 0.0929 mL 0.4646 mL 0.9292 mL 2.3229 mL
30 mM 0.0774 mL 0.3871 mL 0.7743 mL 1.9357 mL
40 mM 0.0581 mL 0.2904 mL 0.5807 mL 1.4518 mL
50 mM 0.0465 mL 0.2323 mL 0.4646 mL 1.1614 mL
60 mM 0.0387 mL 0.1936 mL 0.3871 mL 0.9679 mL
80 mM 0.0290 mL 0.1452 mL 0.2904 mL 0.7259 mL
100 mM 0.0232 mL 0.1161 mL 0.2323 mL 0.5807 mL
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CDK8/19-IN-1 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.

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Product Name:
CDK8/19-IN-1
Cat. No.:
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