product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
3605/10
catalog :
3605/10
quantity :
10 mg
price :
335 USD
more info or order :
citations: 8
Reference
Słabicki M, Kozicka Z, Petzold G, Li Y, Manojkumar M, Bunker R, et al. The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K. Nature. 2020;: pubmed publisher
Malonia S, Dutta P, Santra M, Green M. F-box protein FBXO31 directs degradation of MDM2 to facilitate p53-mediated growth arrest following genotoxic stress. Proc Natl Acad Sci U S A. 2015;112:8632-7 pubmed publisher
Wu J, Zhao Z, Sabirzhanov B, Stoica B, Kumar A, Luo T, et al. Spinal cord injury causes brain inflammation associated with cognitive and affective changes: role of cell cycle pathways. J Neurosci. 2014;34:10989-1006 pubmed publisher
Goonesekere N, Wang X, Ludwig L, Guda C. A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers. PLoS ONE. 2014;9:e93046 pubmed publisher
Wu J, Renn C, Faden A, Dorsey S. TrkB.T1 contributes to neuropathic pain after spinal cord injury through regulation of cell cycle pathways. J Neurosci. 2013;33:12447-63 pubmed publisher
Wu J, Raver C, Piao C, Keller A, Faden A. Cell cycle activation contributes to increased neuronal activity in the posterior thalamic nucleus and associated chronic hyperesthesia after rat spinal cord contusion. Neurotherapeutics. 2013;10:520-38 pubmed publisher
Wu J, Kharebava G, Piao C, Stoica B, Dinizo M, Sabirzhanov B, et al. Inhibition of E2F1/CDK1 pathway attenuates neuronal apoptosis in vitro and confers neuroprotection after spinal cord injury in vivo. PLoS ONE. 2012;7:e42129 pubmed publisher
Wu J, Pajoohesh Ganji A, Stoica B, Dinizo M, Guanciale K, Faden A. Delayed expression of cell cycle proteins contributes to astroglial scar formation and chronic inflammation after rat spinal cord contusion. J Neuroinflammation. 2012;9:169 pubmed publisher
product information
master code :
3605
SKU :
3605/10
product name :
(R)-CR8
unit size :
10 mg
description :
Cdk inhibitor; potently inhibits cdk1 and cdk2; also inhibits CK1; acts as molecular glue
target :
Cyclin-dependent Kinase Inhibitors
category :
Small Molecules
purity :
99%
observed molecular weight :
540.92
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
( 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 M for cdk2, cdk1, cdk5, cdk9 and cdk7, respectively). Also inhibits casein kinase 1 (CK1; IC50 = 0.6 M). 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.
top caption :
Cdk inhibitor; potently inhibits cdk1 and cdk2; also inhibits CK1; acts as molecular glue
extended description :
Cdk inhibitor; potently inhibits cdk1 and cdk2; also inhibits CK1; acts as molecular glue
chemical name text :
(2R)-2-[[9-(Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol trihydrochloride
formula :
C24H29N7O.3HCl
formula text :
C24H29N7O.3HCl
cas num :
1786438-30-9
USD :
335 USD
product details :
Cdk inhibitor; potently inhibits cdk1 and cdk2; also inhibits CK1; acts as molecular glue
storage :
Store at +4░C
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK