GSK321
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 α-Hydroxyglutaric acid (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
1816331-63-1
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/gsk321.html
Concentration
10mM
Purity
99.21
Solubility
DMSO : 250 mg/mL (ultrasonic)
Smiles
O=C(C1=CC=CN1)N2C[C@@H](C)C(N(CC3=CC=C(F)C=C3)N=C4C(NC5=CC([C@H](C)O)=CC=C5)=O)=C4C2
Molecular Formula
C28H28FN5O3
Molecular Weight
501.55
References & Citations
[1]Ujunwa C Okoye-Okafor, 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
4°C (Powder, protect from light)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
Explore Other Products
Browse additional items from our catalog
SRC8, NT (CTTN, EMS1, Src substrate cortactin, Amplaxin, Oncogene EMS1) (Azide free) (HRP) discontinued
Lentiviral human KPTN shRNA (UAS) - Lentiviral human KPTN shRNA (UAS, GFP) (25)
SLITL2 (VASN) (NM_138440) Human Tagged ORF Clone Lentiviral Particle