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

CDK8/19-IN-1 

Cat. No.: HY-111427
Handling Instructions

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

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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].

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].

Storage

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

References
Molecular Weight

430.50

Formula

C₁₉H₁₈N₄O₄S₂

CAS No.

1818427-07-4

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

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CDK8/19-IN-1
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CDK8/19-IN-1

Cat. No.: HY-111427