| Identification | Back Directory | [Name]
2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride | [CAS]
294646-77-8 | [Synonyms]
R8
(R)-CR8
(S)-CR8
CR8, (R)-Isomer
CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem
(R)-2-(1-Hydroxybut-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-iso-propylpurine
2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride
(2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol
(2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-butanol-1
1-Butanol,2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]Methyl]aMino]-9H-purin-2-yl]aMino]-,(2R)- | [Molecular Formula]
C24H29N7O | [MDL Number]
MFCD18785641 | [MOL File]
294646-77-8.mol | [Molecular Weight]
431.53 |
| Chemical Properties | Back Directory | [Melting point ]
98-100℃ | [Boiling point ]
671.4±65.0 °C(Predicted) | [density ]
1.27±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥10mg/mL | [form ]
powder | [pka]
14.56±0.10(Predicted) | [color ]
off-white | [Stability:]
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Hazard Information | Back Directory | [Description]
CR8 (294646-77-8) is a second generation analog of roscovitine which inhibits cyclin-dependent kinases with increased potency, Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk5, p25, and Cdk9/cyclin T, IC50s=0.09, 0.072, 0.041, 0.11 and 0.18 μM respectively.1,2 Acts as a molecular glue degrader that depletes cyclin K.3 CR8 displays neuroprotective effects in various models including traumatic brain injury.4 | [Uses]
CR8, (R)-Isomer is a cell-permeable, ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor. | [Biochem/physiol Actions]
CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). CR8 is a more potent pyridyl analogue of roscovitine (Cat. No. R7772). In comparison to roscovirtine, the compound gains in potency toward CK1, which is involved in amyloid-β formation. The R-CR8 enantiomer is slightly more potent than S. CR8 is around 30 times more potent at cellular assay then roscovitine. Acts as a molecular glue to induce cyclin K degradation. | [storage]
Store at -20°C | [References]
Bettayeb et al. (2008), C8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases; Oncogene, 27 5797
Bettayeb et al. (2010), CDK Inhibitors Roscovitine and CR8 Trigger Mcl-1 Down-Regulation and Apoptotic Cell Death in Neuroblastoma Cells; Genes Cancer, 1 369
Slabiki et al. (2020), The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K; Nature, 585 293
Aubrecht et al. (2018), Comparing effects of CDK inhibitor and E2F1/2 ablation on neuronal cell death pathways in vitro and after traumatic brain injury; Cell Death Dis., 9 112 |
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