GW8510

Name: GW8510
Brand: MedChemExpress
SKU: HY-112358
Rating: 4.5 (1 reviews)

Cat. No.: HY-112358 Purity: 99.04%: Data Sheet
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GW8510 is a potent cyclin-dependent kinase-2 (CDK2) inhibitor. GW8510 is also a ribonucleotide reductase M2 (RRM2) inhibitor. GW8510 exhibits neuroprotective and anticancer activities.

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

GW8510 Chemical Structure

CAS No. : 222036-17-1

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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
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Based on 1 publication(s) in Google Scholar

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View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

Biological Activity
Purity & Documentation
References
Customer Review

Description

GW8510 is a potent cyclin-dependent kinase-2 (CDK2) inhibitor. GW8510 is also a ribonucleotide reductase M2 (RRM2) inhibitor. GW8510 exhibits neuroprotective and anticancer activities^[1]^[2]^[3].

IC₅₀ & Target^[1]^[2]

CDK2

CDK5

RRM2

Cellular Effect

Cell Line	Type	Value	Description	References
HFF	IC₅₀	13 μM Compound: 91	Inhibition of human foreskin fibroblasts (HFF) proliferation Inhibition of human foreskin fibroblasts (HFF) proliferation	[PMID: 11728181]
HT-29	IC₅₀	5.1 μM Compound: 91	Inhibition of HT-29 tumor cell proliferation Inhibition of HT-29 tumor cell proliferation	[PMID: 11728181]
MDA-MB-468	IC₅₀	6.8 μM Compound: 91	Inhibition of MDA-MB468 tumor cell proliferation Inhibition of MDA-MB468 tumor cell proliferation	[PMID: 11728181]
RKO	IC₅₀	1.7 μM Compound: 91	Inhibition of RKO tumor cell proliferation Inhibition of RKO tumor cell proliferation	[PMID: 11728181]
SW-620	IC₅₀	10 μM Compound: 91	Inhibition of SW620 tumor cell proliferation Inhibition of SW620 tumor cell proliferation	[PMID: 11728181]
Sf9	IC₅₀	0.003 μM Compound: GW8510	Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.007 μM Compound: GW8510	Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.049 μM Compound: GW8510	Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.139 μM Compound: GW8510	Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.317 μM Compound: GW8510	Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.54 μM Compound: GW8510	Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]

In Vitro

GW8510 (0.5-4 μM; 72 h) inhibits viability of HCT116 cells in a dose-dependent manner^[2].
GW8510 (1-4 μM; 24 h) inhibits RRM2 expression without alteration of RRM1 expression^[2].
GW8510 inhibits CDK2 and other CDKs when tested in in vitro biochemical assays, when used on cultured neurons it only inhibits CDK5^[1].
GW8510 inhibits the death of cerebellar granule neurons caused by switching them from high potassium medium to low potassium medium^[1].
Combination with GW8510 (5 μM; 48 h) and Tamoxifen (5 μM; 48 h) significantly inhibits survival of the Tamoxifen-resistant breast cancer cells (BBCs) through induction of autophagic cell death^[3].

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

Cell Viability Assay^[2]

Cell Line:	HCT116 cells
Concentration:	0.5, 1, 2, 4 μM
Incubation Time:	72 hours
Result:	Inhibited HCT116 cells growth.

Western Blot Analysis^[2]

Cell Line:	HCT116 cells
Concentration:	1, 2, 4 μM
Incubation Time:	24 hours
Result:	Inhibited RRM2 expression. The reduction of RRM2 protein level can be reversed by MG132.

In Vivo

Combination with GW8510 and Tamoxifen enhances tumoricidal effect on Tamoxifen-resistant BBC xenograft through autophagy induction^[3].

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

Molecular Weight

449.51

Formula

C₂₁H₁₅N₅O₃S₂

CAS No.

222036-17-1

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(C1=CC=C(N/C=C(C2=C(SC=N3)C3=CC=C2N4)\C4=O)C=C1)(NC5=NC=CC=C5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (55.62 mM; Need ultrasonic; 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	2.2246 mL	11.1232 mL	22.2464 mL
5 mM	0.4449 mL	2.2246 mL	4.4493 mL
10 mM	0.2225 mL	1.1123 mL	2.2246 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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Concentration _(final)

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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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.04%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (258 KB) HNMR (277 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. ARCAMONE F, et, al. STRUCTURE AND SYNTHESIS OF DISTAMYCIN A. Nature. 1964 Sep 5;203:1064-5. [Content Brief]

[2]. Hiraku Y, et, al. Distamycin A, a minor groove binder, changes enediyne-induced DNA cleavage sites and enhances apoptosis. Nucleic Acids Res Suppl. 2002;(2):95-6. [Content Brief]

[3]. Majumder P, et, al. Effect of DNA groove binder distamycin A upon chromatin structure. PLoS One. 2011;6(10):e26486. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2246 mL	11.1232 mL	22.2464 mL	55.6161 mL
	5 mM	0.4449 mL	2.2246 mL	4.4493 mL	11.1232 mL
	10 mM	0.2225 mL	1.1123 mL	2.2246 mL	5.5616 mL
	15 mM	0.1483 mL	0.7415 mL	1.4831 mL	3.7077 mL
	20 mM	0.1112 mL	0.5562 mL	1.1123 mL	2.7808 mL
	25 mM	0.0890 mL	0.4449 mL	0.8899 mL	2.2246 mL
	30 mM	0.0742 mL	0.3708 mL	0.7415 mL	1.8539 mL
	40 mM	0.0556 mL	0.2781 mL	0.5562 mL	1.3904 mL
	50 mM	0.0445 mL	0.2225 mL	0.4449 mL	1.1123 mL

GW8510 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:

GW8510222036-17-1GW 8510GW-8510CDKCyclin dependent kinaseribonucleotide reductase M2RRM2neuroprotectiveanticancerInhibitorinhibitorinhibit

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GW8510

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GW8510 Related Antibodies

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Complete Stock Solution Preparation Table

GW8510 Related Classifications

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