JH-XI-10-02
- CAS No.
- 2209085-22-1
- Chemical Name:
- JH-XI-10-02
- Synonyms
- JH-X1-10-02;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-
- CBNumber:
- CB54844926
- Molecular Formula:
- C53H69N5O9
- Molecular Weight:
- 920.16
- MDL Number:
- MFCD31813655
- MOL File:
- 2209085-22-1.mol
JH-XI-10-02 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-0042316 | JH-XI-10-02 98.18% | 2209085-22-1 | 1mg | $580 | 2021-12-16 | Buy |
ChemScene | CS-0042316 | JH-XI-10-02 98.18% | 2209085-22-1 | 5mg | $1450 | 2021-12-16 | Buy |
ChemScene | CS-0042316 | JH-XI-10-02 98.18% | 2209085-22-1 | 10mg | $2350 | 2021-12-16 | Buy |
ChemScene | CS-0042316 | JH-XI-10-02 98.18% | 2209085-22-1 | 25mg | $4500 | 2021-12-16 | Buy |
JH-XI-10-02 Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
JH-XI-10-02 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9708 | 58 |
Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9863 | 58 |
Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9730 | 58 |
Jilin Province Woda Biotechnology Co., Ltd. | 13504435624 | 1927928688@qq.com | China | 1366 | 58 |
ShangHai ChuanQian Chemcial Technique Centre | 15869524721 | 3525679403@qq.com | China | 3617 | 58 |
cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 10011 | 58 |
Changzhou Bojia Biomedical Technology Co., Ltd. | 2122619822 | czbjpharma@126.com | China | 18488 | 58 |