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

Cat. No.: HY-18340A Purity: 98.95%: FAQs
Data Sheet SDS COA 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

CAS No. : 1786438-30-9

Size	Price	Stock	Quantity

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10 mM * 1 mL in DMSO	USD 179	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL ready for reconstitution	USD 179	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1090	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1900	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of (R)-CR8 trihydrochloride:

(R)-CR8 In-stock

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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

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

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:	5 mg/Kg
Administration:	i.p.
Result:	Resulted in a significant reduction in lesion size.

Clinical Trial

Molecular Weight

540.92

Appearance

Solid

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.[H]Cl.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (92.44 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 available by MCE.

Purity & Documentation

Purity: 98.95%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (253 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

[1]. Bettayeb K, et al. CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene. 2008 Oct 2;27(44):5797-807. [Content Brief]

[2]. Kabadi SV, et al. CR8, a novel inhibitor of CDK, limits microglial activation, astrocytosis, neuronal loss, and neurologic dysfunction after experimental traumatic brain injury. J Cereb Blood Flow Metab. 2014 Mar;34(3):502-13. [Content Brief]

[3]. Słabicki M, et al. The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K [published online ahead of print, 2020 Jun 3]. Nature. 2020;10.1038/s41586-020-2374-x. [Content Brief]

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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Keywords:

(R)-CR8 trihydrochloride1786438-30-9CR8, (R)-Isomer trihydrochlorideMolecular GluesCDKApoptosisCyclin dependent kinasecelldeathapoptosisneuroprotectivelesionHippocampusPARPcaspasesInhibitorinhibitorinhibit

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

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Other Forms of (R)-CR8 trihydrochloride:

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