GW296115 |
Catalog No.GC81304
One-Click Copy Product Info
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GW296115 is a multi-target inhibitor with the following IC50 values against its targets: 8.4 nM for BRSK2, 21 nM for BRSK1, 1.8 μM for PDGFRβ, 5.5 nM for STK17B/DRAK2, 28 nM for DRAK1, 20 nM for PHKG1, and 89 nM for DCAMKL3.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 118458-58-5
Sample solution is provided at 25 µL, 10mM.
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In Vitro, GW296115 (1 μM) inhibits 25 out of 403 wild-type human kinases by over 90% at a concentration of 1 μM, with a selectivity index of 0.062[1]. GW296115 potently inhibits 6 IDG dark kinases in enzymatic assays, with IC50 values ranging from 5.5 nM (DRAK2) to 89 nM (DCAMKL3)[1]. GW296115 (1 μM; 72 h) exerts no effect on cell proliferation in 17 tested cancer cell lines and normal cell lines (including non-malignant MCF10A and MRC-5) following treatment at 1 μM for 72 h[1]. GW296115 (incubated for 2 h) potently binds to BRSK2 in living HEK293 cells with an IC50 of 107 nM, confirming that it is a cell-active BRSK2 inhibitor[1]. GW296115 (2.5 μM; 2-6 h) abolishes BRSK2-induced phosphorylation of AMPK substrates in HEK293T cells (this effect is observed at both 2 h and 6 h) and induces hyperphosphorylation of BRSK2 at the T174 site[1]. GW296115 (2-5 μM) inhibits autophagy and enhances apoptosis in MDA-MB-231 triple-negative breast cancer cells, while it also inhibits autophagy and enhances apoptosis in BT-474 estrogen receptor-positive breast cancer cells[2]. GW296115 (2 μM; 24 h) inhibits the growth of MDA-MB-231 triple-negative breast cancer cells[2]. GW296115 (2-3 μM; 72 h) reduces the 3D invasiveness of MDA-MB-231 triple-negative breast cancer cells[2].
References:
[1]. Tamir TY, et al. PKIS deep dive yields a chemical starting point for dark kinases and a cell active BRSK2 inhibitor. Sci Rep. 2020 Sep 28;10(1):15826.
[2]. Maiti A, et al. BRSK2 plays a role in autophagy and cancer cell growth and survival under nutrient deprivation stress via the PIK3C3 pathway. Sci Rep. 2025 Nov 19;15(1):40651.
| Cas No. | 118458-58-5 | SDF | |
| Formula | C22H15N3O4 | M.Wt | 385.37 |
| Solubility | DMSO: 50 mg/mL (129.75 mM; Need ultrasonic) | Storage | Store at 4°C, away from moisture |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5949 mL | 12.9745 mL | 25.9491 mL |
| 5 mM | 519 μL | 2.5949 mL | 5.1898 mL |
| 10 mM | 259.5 μL | 1.2975 mL | 2.5949 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)