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JH-XI-10-02

SKU: orb2655763

Description

JH-XI-10-02 is a CDK8 PROTAC based on the CDK8 inhibitor JH-VIII-49, induces partial degradation of CDK8 in Jurkat cells with IC50 of 159 nM.

Images & Validation

Key Properties

CAS Number2209085-22-1
MW920.161
Purity>98% (HPLC)
FormulaC53H69N5O9
SMILESCC12CCC(CC1CCC3C2CCC4(C3CCC4C5=CC6=C(C=C5)C=CN=C6)C)N(C)C(=O)CCOCCOCCOCCOCCNC7=CC=CC8=C7C(=O)N(C8=O)C9CCC(=O)NC9=O
TargetPROTAC
SolubilityIn Vitro: DMSO : 100 mg/mL (108.68 mM)

Bioactivity

In Vitro
Western blot analysis. Cell line: Jurkat cells. Concentration: 1 μM. Incubation time: 6 and 24 hours. Result: Partial degradation of CDK8 upon treatment for 6 h at a concentration of 1 μM. Significant degradation of CDK8 after treatment for 24 h at a concentration of 1 μM. Western blot analysis. Cell line: WT Molt4 and CRBN null Molt4 cells. Concentration: 0.1, 0.5, 1, 2, 5 μM Incubation time: 24 hours. Result: Degradation of CDK8 at 5 μM in WT Molt4 cells. There were no degradation in CRBN null Molt4 cells at any concentration.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Protocol Information