JH-XI-10-02 - ≥98% , CAS No.2209085-22-1

CAS: 2209085-22-1 Cat. No.: J647710 Molecular Weight: 920.14 PubChem CID: 133081965

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Application

PROTAC

Overview

JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK . JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC 50 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

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. 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. JH-XI-10-02 induces degradation of CDK8 at 5 μM in WT Molt4 cells, no degradation in CRBN 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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 AnalysisCell Line: WT Molt4 and CRBN 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 Molt4 cells at any concentration.

Form:Solid

IC50& Target:CDK8 159 nM (IC 50 ) Cereblon

Specifications

Specifications & Purity

≥98%

Biochemical and Physiological Mechanisms

JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK . JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC 50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Purity

≥98%

Names and Identifiers

• Canonical Smiles: CC12CCC(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
• IUPAC Name: 3-[2-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethoxy]-N-[(3S,8R,10S,13S,14S,17S)-17-isoquinolin-7-yl-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl]-N-methylpropanamide
• InChIKey: JECHBTRAPARMGI-KMIZWFMDSA-N
• INCHI: 1S/C53H69N5O9/c1-52-19-15-38(32-37(52)9-10-39-42-12-11-41(53(42,2)20-16-43(39)52)35-8-7-34-17-21-54-33-36(34)31-35)57(3)47(60)18-23-64-25-27-66-29-30-67-28-26-65-24-22-55-44-6-4-5-40-48(44)51(63)58(50(40)62)45-13-14-46(59)56-49(45)61/h4-8,17,21,31,33,37-39,41-43,45,55H,9-16,18-20,22-30,32H2,1-3H3,(H,56,59,61)/t37?,38-,39-,41+,42-,43?,45?,52-,53+/m0/s1
• PubChem CID: 133081965
• Molecular Weight: 920.14

Chemical and Physical Properties

• Solubility: DMSO : 100 mg/mL (108.68 mM; Need ultrasonic)