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

JH-XI-10-02 

Cat. No.: HY-111518 Purity: 98.18%
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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1 mg USD 580 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 2350 In-stock
Estimated Time of Arrival: December 31
25 mg USD 4500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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.
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 : 100 mg/mL (108.68 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0868 mL 5.4340 mL 10.8679 mL
5 mM 0.2174 mL 1.0868 mL 2.1736 mL
10 mM 0.1087 mL 0.5434 mL 1.0868 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5.75 mg/mL (6.25 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
JH-XI-10-02
Cat. No.:
HY-111518
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