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Description: Cdk inhibitor; potently inhibits cdk1 and cdk2; also inhibits CK1; acts as molecular glue
Chemical Name: (2R)-2-[[9-(Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol trihydrochloride
Purity: ≥99% (HPLC)
Citations (7)

Biological Activity for (R)-CR8

(R)-CR8 is a cyclin dependent kinase (cdk) inhibitor (reported IC50 values are 0.036 - 0.07, 0.09 - 0.8, 0.13 - 0.68, 0.18 - 1 and >1 μM for cdk2, cdk1, cdk5, cdk9 and cdk7, respectively). Also inhibits casein kinase 1 (CK1; IC50 = 0.6 μM). Acts as molecular glue; forms a complex between CDK12-cyclin K and the CUL4 adapter protein DDB1 resulting in ubiquination and degradation of cyclin K.

Compound Libraries for (R)-CR8

(R)-CR8 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for (R)-CR8

M. Wt 540.92
Formula C24H29N7O.3HCl
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 1786438-30-9
PubChem ID 90488866
Smiles CC(C)N2C1=NC(N[C@H](CC)CO)=NC(NCC3=CC=C(C4=NC=CC=C4)C=C3)=C1N=C2.Cl.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for (R)-CR8

Solvent Max Conc. mg/mL Max Conc. mM
water 54.09 100
DMSO 54.09 100

Preparing Stock Solutions for (R)-CR8

The following data is based on the product molecular weight 540.92. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.85 mL 9.24 mL 18.49 mL
5 mM 0.37 mL 1.85 mL 3.7 mL
10 mM 0.18 mL 0.92 mL 1.85 mL
50 mM 0.04 mL 0.18 mL 0.37 mL

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Product Datasheets for (R)-CR8

Certificate of Analysis / Product Datasheet
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References for (R)-CR8

References are publications that support the biological activity of the product.

Oumata et al (2008) Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1. J.Med.Chem. 51 5229 PMID: 18698753

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987

Słabicki et al (2020) The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K. Nature 585 293 PMID: 32494016

If you know of a relevant reference for (R)-CR8, please let us know.

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Keywords: (R)-CR8, (R)-CR8 supplier, cdk1, cdk5, inhibitors, inhibits, CK1, cyclin-dependent, kinases, casein, kinase, 1, Cyclin-dependent, Kinase, Casein, Molecular, Glues, Non-selective, CDKs, 3605, Tocris Bioscience

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