[CAS NO. 222036-17-1] GW8510
PRODUCTS SPECIFICATIONS [222036-17-1]
DESCRIPTION [222036-17-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 449.51 |
| Molecular Formula | C21H15N5O3S2 |
| 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 |
Summary
IC50 & Target
|
CDK2 |
CDK5 |
RRM2 |
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]
.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
- [1] ARCAMONE F, et, al. STRUCTURE AND SYNTHESIS OF DISTAMYCIN A. Nature. 1964 Sep 5;203:1064-5.
- [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.
- [3] Majumder P, et, al. Effect of DNA groove binder distamycin A upon chromatin structure. PLoS One. 2011;6(10):e26486.