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(R)-CR8

Chemical Structure : (R)-CR8

CAS No.: 294646-77-8

(R)-CR8 (CR8 R-isomer, CR8)

Catalog No.: PC-38299Not For Human Use, Lab Use Only.

(R)-CR8 is a potent CDK1/2/5/7/9 inhibitor, inhibits CDK1/cyclin B (IC50, 90 nM), CDK2/cyclin A (72 nM), CDK2/cyclin E (41 nM), CDK5/p25 ( 110 nM), CDK7/cyclin H (1.1 uM), CDK9/cyclin T (0.18 uM) and CK1δ/ε (0.4 uM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

(R)-CR8 (CR8) is a potent CDK1/2/5/7/9 inhibitor, inhibits CDK1/cyclin B (IC50, 90 nM), CDK2/cyclin A (72 nM), CDK2/cyclin E (41 nM), CDK5/p25 ( 110 nM), CDK7/cyclin H (1.1 uM), CDK9/cyclin T (0.18 uM) and CK1δ/ε (0.4 uM).
(R)-CR8 induces apoptosis and has neuroprotective effect.
CR8 binds CDK12-cyclin K and recruits the DDB1–CUL4–RBX1 E3 ligase core to ubiquitinate cyclin K
(R)-CR8 also acts as a molecular glue degrader that depletes cyclin K.

Physicochemical Properties

M.Wt 431.544
Formula C24H29N7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-butanol-1

References

1. Słabicki M, et al. Nature. 2020 Sep;585(7824):293-297.

2. Huang BY, et al. CNS Neurosci Ther. 2019 May;25(5):612-620. 

3. Husson H, et al. Hum Mol Genet. 2016 Jun 1;25(11):2245-2255.

4. Delehouzé C, et al. Oncogene. 2014 Dec 11;33(50):5675-87.

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