製品番号: HY-18340

(R)?-?CR8

Name: (R)?-?CR8
Brand: MedChemExpress
SKU: HY-18340
Price: 180.00 USD
Availability: InStock
Rating: 5 (3 reviews)

(別名: CR8, (R)-Isomer)

3 Cited Publications

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

(R)-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.

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純度 : 99.52%
CAS 番号: 294646-77-8
分子式: C₂₄H₂₉N₇O
分子量:431.53

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

(R)-CR8 構造式

CAS 番号: 294646-77-8

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数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (3)
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

(R)-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)

CDK アイソフォーム固有の製品をすべて表示 :

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 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	0.062 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	0.225 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]

体外実験

(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.

体内実験

(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.

Related Protocols :

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 294646-77-8
性状 Solid
分子量 431.53
分子式 C₂₄H₂₉N₇O
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
別名

CR8, (R)-Isomer
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

Publications (3)

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Sci Adv

Cyclin K condensates bridge CDK12 to phosphorylate and drive oncogenic YAP activation in hepatocellular carcinoma. [Abstract]

2026 Jul 3;12(27):eaec6492. PMID: 42397909
Mol Cancer Ther

2026 Aug 13. PMID: 42594405
Structure

CAND1 and CAND2 drive CUL4 substrate receptor exchange with largely comparable biochemical efficiency, unlike their relative effects on CUL1. [Abstract]

2026 Mar 20:S0969-2126(26)00056-0. PMID: 41864201

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

(R)-CR8

3 Cited Publications

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(R)?-?CR8

MedChemExpress（MCE）の使用を引用している文献 (R)-CR8

CDK アイソフォーム固有の製品をすべて表示

生物活性