(R)-CR8 (trihydrochloride)

$90$745

Products Details

Product Description

– (R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect[1][2]. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K[3].

Web ID

– HY-18340A

Storage Temperature

– 4°C (Powder, sealed storage, away from moisture)

Shipping

– Room Temperature

Applications

– Cancer-Kinase/protease

Molecular Formula

– C24H32Cl3N7O

References

– [1]Bettayeb K, et al. CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene. 2008 Oct 2;27(44):5797-807.|[2]Kabadi SV, et al. CR8, a novel inhibitor of CDK, limits microglial activation, astrocytosis, neuronal loss, and neurologic dysfunction after experimental traumatic brain injury. J Cereb Blood Flow Metab. 2014 Mar;34(3):502-13.|[3]SÅ‚abicki M, et al. The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K [published online ahead of print, 2020 Jun 3]. Nature. 2020;10.1038/s41586-020-2374-x.

CAS Number

– 1786438-30-9

Molecular Weight

– 540.92

Compound Purity

– 98.95

SMILES

– CC[C@@H](NC1=NC(NCC2=CC=C(C3=NC=CC=C3)C=C2)=C4N=CN(C(C)C)C4=N1)CO.[H]Cl.[H]Cl.[H]Cl

Clinical Information

– No Development Reported

Research Area

– Cancer; Neurological Disease

Solubility

– DMSO : 50 mg/mL (ultrasonic)

Target

– Apoptosis;CDK;Molecular Glues

Isoform

– CDK1;CDK2;CDK5;CDK7;CDK9

Pathway

– Apoptosis;Cell Cycle/DNA Damage;PROTAC

Product type

– Reference compound

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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