1. Cell Cycle/DNA Damage
    Apoptosis
  2. CDK
    Apoptosis
  3. (R)​-​CR8

(R)​-​CR8 (Synonyms: CR8, (R)-Isomer)

Cat. No.: HY-18340 Purity: >98.0%
Handling Instructions

(R)​-​CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)​-​CR8 (CR8) 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 (CR8) induces apoptosis and has neuroprotective effect.

For research use only. We do not sell to patients.

(R)​-​CR8 Chemical Structure

(R)​-​CR8 Chemical Structure

CAS No. : 294646-77-8

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10 mM * 1  mL in DMSO USD 522 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 990 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

(R)​-​CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)​-​CR8 (CR8) 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 (CR8) induces apoptosis and has neuroprotective effect[1][2].

IC50 & Target[1]

Cdk1/cyclin B

0.09 μM (IC50)

cdk2/cyclin A

0.072 μM (IC50)

CDK2/cyclinE

0.041 μM (IC50)

Cdk5/p25

0.11 μM (IC50)

CDK7/cyclin H

1.1 μM (IC50)

CDK9/Cyclin T

0.18 μM (IC50)

CK1δ/ε

0.4 μM (IC50)

In Vitro

(R)-CR8 (CR8) (0.1-100 μM; 48 hours) is a potent inducer of apoptotic cell death with an IC50 of 0.49 μM for SH-SY5Y cell line[1].
(R)-CR8 (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage[1].

Apoptosis Analysis[1]

Cell Line: SH-SY5Y cell line
Concentration: 0.1, 1, 10, 100 μM
Incubation Time: 24 hours
Result: Reduced cell survival in a dose-dependent manner.
In Vivo

(R)-CR8 (5 mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment[2].

Animal Model: Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330 g)[2]
Dosage: i.p.
Administration: 5 mg/Kg
Result: Resulted in a significant reduction in lesion size.
Clinical Trial
Molecular Weight

431.53

Formula

C₂₄H₂₉N₇O

CAS No.

294646-77-8

SMILES

CC[[email protected]@H](NC1=NC(NCC2=CC=C(C3=NC=CC=C3)C=C2)=C4N=CN(C(C)C)C4=N1)CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
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Keywords:

(R)​-​CR8CR8, (R)-IsomerCDKApoptosisCyclin dependent kinasecelldeathapoptosisneuroprotectivelesionHippocampusPARPcaspasesInhibitorinhibitorinhibit

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