(S, R) -GSK321
(S, R) -GSK321 is the (S, R) -enantiomer of GSK321 (HY-18948) . GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. GSK321can be used for research of acute myeloid leukemia (AML) and other cancers[1].
Product Specifications
CAS Number
[1816272-18-0]
UNSPSC
12352005
Target
Isocitrate Dehydrogenase (IDH)
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/s-r-gsk321.html
Purity
98.62
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
C[C@@H](O)C1=CC=CC(NC(C2=NN(C3=C2CN(C[C@@H]3C)C(C4=CC=CN4)=O)CC5=CC=C(C=C5)F)=O)=C1
Molecular Formula
C28H28FN5O3
Molecular Weight
501.55
References & Citations
[1]Okoye-Okafor UC, et, al. New IDH1 mutant inhibitors for treatment of acute myeloid leukemia. Nat Chem Biol. 2015 Nov;11 (11) :878-86.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
IDH1
Available Sizes
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