| Company Name: |
Shanghai Chaolan Chemical Technology Center
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QQ:65489617 15618227136 |
| Email: |
info@SuperLan-chem.com |
| Products Intro: |
Product Name:JH-XI-10-02
CAS:2209085-22-1
Purity:98% HPLC Package:5MG;10MG;50MG;100MG,1G,5G,500G
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| | JH-XI-10-02 Basic information |
| Product Name: | JH-XI-10-02 | | Synonyms: | 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-;JH-XI-10-02;JH-X1-10-02 | | CAS: | 2209085-22-1 | | MF: | C53H69N5O9 | | MW: | 920.16 | | EINECS: | | | Product Categories: | | | Mol File: | 2209085-22-1.mol |  |
| | JH-XI-10-02 Chemical Properties |
| density | 1.28±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (108.68 mM; Need ultrasonic) | | pka | 10.74±0.40(Predicted) | | form | Solid | | color | Yellow to brown |
| | JH-XI-10-02 Usage And Synthesis |
| 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. |
| | JH-XI-10-02 Preparation Products And Raw materials |
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