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

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

Cat. No.: HY-18340 Purity: 99.21%
COA Handling Instructions

(R)​-​CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)​-​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 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.

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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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 198 In-stock
Solution
10 mM * 1 mL in DMSO USD 198 In-stock
Solid
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10 mg USD 270 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of (R)​-​CR8:

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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 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 induces apoptosis and has neuroprotective effect[1][2]. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K[3].

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].
The CDK-bound form of (R)-CR8 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[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

White to off-white

SMILES

CC[C@@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
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (115.87 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3173 mL 11.5867 mL 23.1734 mL
5 mM 0.4635 mL 2.3173 mL 4.6347 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.21%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3173 mL 11.5867 mL 23.1734 mL 57.9334 mL
5 mM 0.4635 mL 2.3173 mL 4.6347 mL 11.5867 mL
10 mM 0.2317 mL 1.1587 mL 2.3173 mL 5.7933 mL
15 mM 0.1545 mL 0.7724 mL 1.5449 mL 3.8622 mL
20 mM 0.1159 mL 0.5793 mL 1.1587 mL 2.8967 mL
25 mM 0.0927 mL 0.4635 mL 0.9269 mL 2.3173 mL
30 mM 0.0772 mL 0.3862 mL 0.7724 mL 1.9311 mL
40 mM 0.0579 mL 0.2897 mL 0.5793 mL 1.4483 mL
50 mM 0.0463 mL 0.2317 mL 0.4635 mL 1.1587 mL
60 mM 0.0386 mL 0.1931 mL 0.3862 mL 0.9656 mL
80 mM 0.0290 mL 0.1448 mL 0.2897 mL 0.7242 mL
100 mM 0.0232 mL 0.1159 mL 0.2317 mL 0.5793 mL
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(R)​-​CR8 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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