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

(R)​-​CR8 trihydrochloride (Synonyms: CR8, (R)-Isomer trihydrochloride)

Cat. No.: HY-18340A Purity: 99.02%
Handling Instructions

(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. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.

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

(R)​-​CR8 trihydrochloride Chemical Structure

(R)​-​CR8 trihydrochloride Chemical Structure

CAS No. : 1786438-30-9

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of (R)​-​CR8 trihydrochloride:

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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].

IC50 & Target[1]

CDK1/cyclinB1

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) trihydrochloride (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 trihydrochloride (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage[1].
The CDK-bound form of (R)-CR8 trihydrochloride has a solvent-exposed pyridyl moiety that induces the formation of a complex between CDK12-cyclin K and the CUL4 adaptor protein DDB1, bypassing the requirement for a substrate receptor and presenting cyclin K for ubiquitination and degradation

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 trihydrochloride (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: 5 mg/Kg
Administration: i.p.
Result: Resulted in a significant reduction in lesion size.
Clinical Trial
Molecular Weight

540.92

Formula

C₂₄H₃₂Cl₃N₇O

CAS No.

1786438-30-9

SMILES

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

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
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (115.54 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8487 mL 9.2435 mL 18.4870 mL
5 mM 0.3697 mL 1.8487 mL 3.6974 mL
10 mM 0.1849 mL 0.9244 mL 1.8487 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (4.01 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (4.01 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (4.01 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.02%

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Keywords:

(R)​-​CR8 trihydrochlorideCR8, (R)-Isomer trihydrochlorideCDKApoptosisCyclin dependent kinasecelldeathapoptosisneuroprotectivelesionHippocampusPARPcaspasesInhibitorinhibitorinhibit

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(R)​-​CR8 trihydrochloride
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