JH-XI-10-02
- Product Name
- JH-XI-10-02
- CAS No.
- 2209085-22-1
- Chemical Name
- JH-XI-10-02
- Synonyms
- JH-XI-10-02;JH-X1-10-02;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-;N-[(1S,3aS,3bR,5aS,7S,9aS,9bS,11aS)-1-(isoquinolin-7-yl)-9a,11a-dimethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-7-yl]-1-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}-N-methyl-3,6,9,12-tetraoxapentadecan-15-amide
- CBNumber
- CB54844926
- Molecular Formula
- C53H69N5O9
- Formula Weight
- 920.16
- MOL File
- 2209085-22-1.mol
JH-XI-10-02 Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-0042316
- Product name
- JH-XI-10-02
- Purity
- 98.18%
- Packaging
- 1mg
- Price
- $580
- Updated
- 2021/12/16
- Product number
- CS-0042316
- Product name
- JH-XI-10-02
- Purity
- 98.18%
- Packaging
- 5mg
- Price
- $1450
- Updated
- 2021/12/16
- Product number
- CS-0042316
- Product name
- JH-XI-10-02
- Purity
- 98.18%
- Packaging
- 10mg
- Price
- $2350
- Updated
- 2021/12/16
- Product number
- CS-0042316
- Product name
- JH-XI-10-02
- Purity
- 98.18%
- Packaging
- 25mg
- Price
- $4500
- Updated
- 2021/12/16
JH-XI-10-02 Chemical Properties,Usage,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
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