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Catalog:
SLK-S8961
Brand:
Selleck
CAS:
1637771-14-2
Overview
MDL
-
Molecular Weight
437.49
Molecular Formula
C26H23N5O2
SMILES
-
For research use only.
Storage
3 years,-20°C,powder 1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
2.2858 mL
11.4288 mL
22.8577 mL
5 mM
0.4572 mL
2.2858 mL
4.5715 mL
10 mM
0.2286 mL
1.1429 mL
2.2858 mL
50 mM
0.0457 mL
0.2286 mL
0.4572 mL
Description
Alobresib (GS-5829) is a novel inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell through deregulation of key signaling pathways, such as , , , and . Alobresib (GS-5829) also inhibits signaling.
Targets
In vitro
In-vitro experiments demonstrates high sensitivity of USC cell-lines to the exposure to GS-5829 causing a dose-dependent decrease in the phosphorylated levels of c-Myc and a dose-dependent increase in caspase activation (apoptosis). GS-5829 inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. IκBα modulation indicates that GS-5829 also inhibits NF-κB signaling. GS-5829-induced apoptosis results from an imbalance between positive (BIM) and negative regulators (BCL-XL) of the intrinsic apoptosis pathway.
