SGC0946 (TFA)

SGC0946 TFA is a selective DOT1L inhibitor with an IC50 value of 0.3 nM. By inhibiting DOT1L, SGC0946 TFA can induce G1 phase arrest, suppress cell self-renewal and metastatic potential, and induce cell differentiation in cancer cells. SGC0946 TFA can be used in the research of tumors such as leukemia and breast cancer, and also serves as a probe to further investigate the cellular mechanisms of DOT1L in normal and diseased cells[1][2][3].

Product Specifications

UNSPSC

12352005

Target

Histone Methyltransferase

Related Pathways

Epigenetics

Field of Research

Cancer

Smiles

CC(C)(C1=CC=C(C=C1)NC(NCCCN(C[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C4=C(C(Br)=C3)C(N)=NC=N4)O2)C(C)C)=O)C.O=C(C(F)(F)F)O

Molecular Formula

C30H41BrF3N7O6

Molecular Weight

732.59

References & Citations

[1]Zhang L, et al. Inhibition of histone H3K79 methylation selectively inhibits proliferation, self-renewal and metastatic potential of breast cancer. Oncotarget. 2014 Nov 15;5 (21) :10665-77.|[2]Zhang X, et al. Prognostic and therapeutic value of disruptor of telomeric silencing-1-like (DOT1L) expression in patients with ovarian cancer. J Hematol Oncol. 2017 Jan 23;10 (1) :29.|[3]Yu W, et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288.