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

Name: (R)-CR8
Brand: MedChemExpress
SKU: HY-18340
Rating: 4.5 (1 reviews)

Cat. No.: HY-18340 Purity: 99.61%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

(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

CAS No. : 294646-77-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	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:

(S)-CR8 Get quote
(R)-CR8 trihydrochloride Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

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)

Cellular Effect

Cell Line	Type	Value	Description	References
G-361	IC₅₀	0.503 μM Compound: CR8	Cytotoxicity against human G361 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay Cytotoxicity against human G361 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay	[PMID: 26851505]
HCT-116	IC₅₀	0.35 μM Compound: CR8	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay	[PMID: 26851505]
HEK293	IC₅₀	0.56 μM Compound: 8m, (R)-C&R8	Antiproliferative activity against HEK293 cells assessed as survival after 48 hrs by MTS reduction assay Antiproliferative activity against HEK293 cells assessed as survival after 48 hrs by MTS reduction assay	[PMID: 18698753]
HT	GI₅₀	0.263 μM Compound: CR8	Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
K562	IC₅₀	0.175 μM Compound: CR8	Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay	[PMID: 26851505]
MCF7	IC₅₀	0.16 μM Compound: CR8	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay	[PMID: 26851505]
Sf9	IC₅₀	0.062 μM Compound: CR8	Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP	[PMID: 30943029]
Sf9	IC₅₀	0.062 μM Compound: CR8	Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP	[PMID: 26851505]
Sf9	IC₅₀	0.225 μM Compound: CR8	Inhibition of recombinant human full-length N-terminal GST-His6 fused CDK5 (M1 to P292 residues)/N-terminal His6-tagged p25 (A104 to R307 residues) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [g Inhibition of recombinant human full-length N-terminal GST-His6 fused CDK5 (M1 to P292 residues)/N-terminal His6-tagged p25 (A104 to R307 residues) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [g	[PMID: 30943029]
Sf9	IC₅₀	0.272 μM Compound: CR8	Inhibition of recombinant human N-terminal GST-His6-fused CDK9 (M1 to F372 residues)/N-terminal His6-tagged cyclin T1 (M1 to K726 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-3 Inhibition of recombinant human N-terminal GST-His6-fused CDK9 (M1 to F372 residues)/N-terminal His6-tagged cyclin T1 (M1 to K726 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-3	[PMID: 30943029]
Sf9	IC₅₀	0.787 μM Compound: CR8	Inhibition of His-tagged CDK1/Cyclin-B1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP Inhibition of His-tagged CDK1/Cyclin-B1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP	[PMID: 30943029]
Sf9	IC₅₀	1.769 μM Compound: CR8	Inhibition of recombinant human N-terminal GST-His6-fused CDK7 (M1 to F346 residues)/N-terminal His-tagged cyclin H (M1 to L323 residues)/N-terminal His6-tagged MAT1 (M1 to S306 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2 Inhibition of recombinant human N-terminal GST-His6-fused CDK7 (M1 to F346 residues)/N-terminal His-tagged cyclin H (M1 to L323 residues)/N-terminal His6-tagged MAT1 (M1 to S306 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2	[PMID: 30943029]
Sf9	IC₅₀	26.09 μM Compound: CR8	Inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 (Q4 to I295 residues) expressed in baculovirus infected Sf9 insect cells using RPPTLSPIPHIPR as substrate measured in presence of [gamma-33P]ATP Inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 (Q4 to I295 residues) expressed in baculovirus infected Sf9 insect cells using RPPTLSPIPHIPR as substrate measured in presence of [gamma-33P]ATP	[PMID: 30943029]
SH-SY5Y	IC₅₀	0.43 μM Compound: 8m, (R)-C&R8	Antiproliferative activity against human SH-SY5Y cells assessed as survival after 48 hrs by MTS reduction assay Antiproliferative activity against human SH-SY5Y cells assessed as survival after 48 hrs by MTS reduction assay	[PMID: 18698753]

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.

294646-77-8

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
10 mM	0.2317 mL	1.1587 mL	2.3173 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.61%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (251 KB) HNMR (253 KB) LCMS (94 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]

Complete Stock Solution Preparation Table

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

(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.

Keywords:

(R)-CR8294646-77-8CR8, (R)-IsomerMolecular GluesCDKApoptosisCyclin dependent kinasecelldeathapoptosisneuroprotectivelesionHippocampusPARPcaspasesInhibitorinhibitorinhibit

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(R)​-​CR8 (Synonyms: CR8, (R)-Isomer)

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(R)​-​CR8 Related Antibodies

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(R)​-​CR8 Related Classifications

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

Other Forms of (R)-CR8:

(R)-CR8 Related Antibodies

(R)-CR8 Related Antibodies

(R)-CR8 Related Classifications