1. Cell Cycle/DNA Damage
  2. CDK
  3. SEL120-34A

SEL120-34A 

Cat. No.: HY-111388
Handling Instructions

SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

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

SEL120-34A Chemical Structure

SEL120-34A Chemical Structure

CAS No. : 1609522-33-9

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Description

SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

IC50 & Target[1]

CDK8/CycC

4.4 nM (IC50)

CDK19/CycC

10.4 nM (IC50)

CDK9/cycT

1070 nM (IC50)

In Vitro

SEL120-34A is a selective, ATP-competitive CDK8 inhibitor, with IC50 of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively. SEL120-34A shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7, and only weakly suppresses CDK9 (IC50, 1070 nM). SEL120-34A is active against a panel of AML cell lines (GI50<1 μM), such as SKNO-1, KG-1, HEL-60, MOLM-16, MV-4-11, OciAML-2, MOLM-6 and OciAML-3 cells, consistent with the effective inhibition range of STAT1 S727 and STAT5 S726[1].

In Vivo

SEL120-34A (30, 60 mg/kg, p.o.) inhibits the growth of tumor in mice bearing MV4-11 cancer cells, and also arrests the growth of KG-1-derived tumors at 30 mg/kg via oral administration[1].

Molecular Weight

414.14

Formula

C₁₅H₁₈Br₂N₄

CAS No.

1609522-33-9

SMILES

CC1=C2C3=C(C(Br)=C1Br)CCCN3C(N4CCNCC4)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

SEL120-34ACDKCyclin dependent kinaseInhibitorinhibitorinhibit

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SEL120-34A
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HY-111388
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