WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407891
Description: JH-XI-10-02 is a potent and selective CDK8 inhibitor. JH-XI-10-02 can recruit the E3 ligase CRL4Cereblon to promote the ubiquitination and proteosomal degradation of CDK8.
MedKoo Cat#: 407891
Chemical Formula: C53H69N5O9
Exact Mass: 919.5095
Molecular Weight: 920.161
Elemental Analysis: C, 69.18; H, 7.56; N, 7.61; O, 15.65
Synonym: JH-XI-10-02; JH-XI10-02; JH-XI 10-02; JH-XI-1002; JH-XI1002; JH-XI 1002; JHXI-1002; JHXI1002; JHXI 1002;
IUPAC/Chemical Name: 1-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-N-((3S,17S)-17-(isoquinolin-7-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-3,6,9,12-tetraoxapentadecan-15-amide
InChi Key: JECHBTRAPARMGI-IBMRIUJRSA-N
InChi Code: 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
SMILES Code: O=C(N([C@H]1CCC2(C)C3CCC4(C)[C@@H](C5=CC6=C(C=C5)C=CN=C6)CCC4C3CCC2C1)C)CCOCCOCCOCCOCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 920.161 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8
John M. Hatcher, Eric S. Wang, Liv Johannessen, Nicholas Kwiatkowski, Taebo Sim and Nathanael S. Gray
Publication Date (Web): March 18, 2018 (Letter)
CDK8 is a cyclin-dependent kinase that forms part of the mediator complex, a multiprotein assembly comprising up to 30 subunits that regulates gene transcription in multiple contexts including stem cell function, immune response, inflammation, cell adhesion, epithelial to mesenchymal transition, and development.