GSK321

• Description :

  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) (HY-113038B), 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].

• 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

• CAS Number :

  [1816331-63-1]