1. PROTAC
    Cell Cycle/DNA Damage
  2. PROTAC
    CDK
  3. JH-XI-10-02

JH-XI-10-02 

Cat. No.: HY-111518
Handling Instructions

JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19.

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

JH-XI-10-02 Chemical Structure

JH-XI-10-02 Chemical Structure

CAS No. : 2209085-22-1

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Description

JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19[1].

IC50 & Target[1]

CDK8

159 nM (IC50)

Cereblon

 

In Vitro

JH-XI-10-02, a bivalent small molecule degrader, recruits the E3 ligase CRL4Cereblon to promote the ubiquitination and proteosomal degradation of CDK8[1].
JH-XI-10-02 (1 μM) induces partial degradation of CDK8 in Jurkat cells upon treatment for 6 h. JH-XI-10-02 (1 μM) induces significant degradation of CDK8 after treatment for 24 h[1].
JH-XI-10-02 induces degradation of CDK8 at 5 μM in WT Molt4 cells, no degradation in CRBN null Molt4 cells at any concentration (0.1-5 μM) in WT Molt4 cells and Molt4 cells where CRBN had been subject to CRISPER/CAS9-mediated deletion for 24 h[1].

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

Western Blot Analysis[1]

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[1]

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.
Molecular Weight

920.14

Formula

C₅₃H₆₉N₅O₉

CAS No.

2209085-22-1

SMILES

O=C(N([[email protected]]1CC[[email protected]]2(C)[[email protected]@]3([H])CC[[email protected]]4(C)[[email protected]@H](C5=CC6=C(C=C5)C=CN=C6)CC[[email protected]@]4([H])[[email protected]]3([H])CC[[email protected]@]2([H])C1)C)CCOCCOCCOCCOCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
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Keywords:

JH-XI-10-02PROTACCDKProteolysis-targeting chimeraCyclin dependent kinaseproteasomaldegradationCDK19CereblonE3 ligaseInhibitorinhibitorinhibit

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JH-XI-10-02
Cat. No.:
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