| Identification | Back Directory | [Name]
JH-XI-10-02 | [CAS]
2209085-22-1 | [Synonyms]
JH-XI-10-02
4,7,10,13-Tetraoxapentadecanamide, 15-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-N-[(3β,5α,17β)-17-(7-isoquinolinyl)androstan-3-yl]-N-methyl- | [Molecular Formula]
C53H69N5O9 | [MDL Number]
MFCD31813655 | [MOL File]
2209085-22-1.mol | [Molecular Weight]
920.16 |
| Chemical Properties | Back Directory | [density ]
1.28±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (108.68 mM; Need ultrasonic) | [form ]
Solid | [pka]
10.74±0.40(Predicted) | [color ]
Yellow to brown |
| Hazard Information | Back Directory | [Biological Activity]
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 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].
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]. | [storage]
Store at -20°C | [References]
[1]. Hatcher JM, et al. Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. ACS Med Chem Lett. 2018 Mar 18;9(6):540-545. |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310 |
| Website: |
http://www.weikeqi-biotech.com/ |
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