SGC0946

SGC0946 is a selective DOT1L inhibitor with an IC50 value of 0.3 nM. By inhibiting DOT1L, SGC0946 can induce G1 phase arrest, suppress cell self-renewal and metastatic potential, and induce cell differentiation in cancer cells. SGC0946 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

CAS Number

[1561178-17-3]

UNSPSC

12352005

Hazard Statement

H301

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/SGC0946.html

Purity

99.68

Solubility

DMSO : 50 mg/mL (ultrasonic)

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

Molecular Formula

C28H40BrN7O4

Molecular Weight

618.57

Precautions

H301

References & Citations

[1]Yu W, et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. |[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]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.