Free shipping on all orders over $ 500

SGC0946

Cat. No. M7578
SGC0946  Structure
Size Price Availability Quantity
10mg USD 135 In stock
50mg USD 500 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

SGC 0946 is over 100-fold selective for other histone methyltransferases/HMTs. SGC 0946 potently reduces H3K79 dimethylation with IC50 of 2.6 nM in A431 cells, and 8.8 nM in MCF10A cells, which potently and selectively kills cells containing an MLL translocation. SGC 0946 is much more potent than its close analog EPZ004777, and serves as an excellent chemical probe for investigating DOT1L and further development of DOT1L inhibitors for cancer therapy.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 618.57
Formula C28H40BrN7O4
CAS Number 1561178-17-3
Purity >98%
Solubility 33 mg/mL in DMSO
Storage at -20°C
References

Tri-methylation of H3K79 is decreased in TGF-β1-induced epithelial-to-mesenchymal transition in lung cancer.
Evanno E, et al. Clin Epigenetics. 2017 Aug 8;9:80. PMID: 28804523.

The Histone Methyltransferase DOT1L Promotes Neuroblastoma by Regulating Gene Transcription.
Wong M, et al. Cancer Res. 2017 May 1;77(9):2522-2533. PMID: 28209620.

Related Histone Methyltransferase Products
WDR5-0103

WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM).

MS023

MS023 is a potent and selective, cell-active inhibitor of type I PRMTs with IC50s of 4-119 nM.

BIX-01294

BIX-01294 is a potent chemical inhibitor of G9a methyltransferase that catalyzes the mono-and di-methylation of the lysine 9 residue of histone H3, with IC50 of 1.9 μM.

EPZ011989

EPZ011989 is a potent, orally-available EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646.

UNC0642

UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SGC0946 supplier, Histone Methyltransferase, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.