SGI-1027, DNMT Inhibitor

Catalog No. size PriceQuantity
M60155-2S 2 mg solid $89
M60155-10S 10mg solid $352


Product Information
Molecular Weight: 461.52
Formula: C27H23N7O
Purity: ≥98%
CAS#: 1020149-73-8
Solubility: DMSO up to 50 mM
Chemical Name: N-(4-((2-amino-6-methylpyrimidin-4-yl)amino)phenyl)-4-(quinolin-4-ylamino)benzamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.


Biological Activity:


SGI-1027 is a potent and selective inhibitor of DNA methyltransferase (DNMT) with IC50 of 6, 8, 7.5 µM for DNMT1, DNMT3A, and DNMT3B. It competes with S-adenosylmethionine in the methylation reaction. Treatment of different cancer cell lines with SGI-1027 resulted in selective degradation of DNMT1 with minimal or no effects on DNMT3A and DNMT3B. SGI-1027 exhibits a moderate pro-apoptotic effect on U937 human leukemia cell line with no relevant changes on the cell cycle. SGI-1027 acts as a novel class of DNA hypomethylating agent that has the potential for use in epigenetic cancer therapy.


How to Use:



  • In vitro: SGI-1027 was used at 10-300 µM final concentration in various in vitro assays.
  • In vivo: n/a




  1. Datta J, et al. A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. (2009) Cancer Res. 69(10):4277-85.
  2. García-Domínguez P, et al. Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line. (2013) Bioorg Med Chem Lett. 23(6):1631-5.
  3. Yoo J, et al. Molecular modeling studies of the novel inhibitors of DNA methyltransferases SGI-1027 and CBC12: implications for the mechanism of inhibition of DNMTs. (2013) PLoS One. 8(4):e62152.
  4. Gamage SA, et al. Structure-activity relationships for 4-anilinoquinoline derivatives as inhibitors of the DNA methyltransferase enzyme DNMT1. (2013) Bioorg Med Chem. 21(11):3147-53.


Products are for research use only. Not for human use.

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed