SGI-1027 --- DNMT Inhibitor


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

Description

SGI-1027 is a potent DNMT inhibitor, which reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. Treatment of different cancer cell lines with SGI-1027 resulted in selective degradation of DNMT1 with minimal or no effects on DNMT3A and DNMT3B. At a concentration of 2.5 to 5 micromol/L (similar to that of decitabine), complete degradation of DNMT1 protein was achieved within 24 h without significantly affecting its mRNA level. SGI-1027 may have the potential for use in epigenetic cancer therapy.

Product information

CAS Number: 1020149-73-8

Molecular Weight: 461.52

Formula: C27H23N7O

Chemical Name: N-(4-((2-amino-6-methylpyrimidin-4-yl)amino)phenyl)-4-(quinolin-4-ylamino)benzamide

Smiles: CC1=CC(NC2C=CC(=CC=2)NC(=O)C2C=CC(=CC=2)NC2=CC=NC3=CC=CC=C23)=NC(N)=N1

InChiKey: QSYLKMKIVWJAAK-UHFFFAOYSA-N

InChi: InChI=1S/C27H23N7O/c1-17-16-25(34-27(28)30-17)32-20-10-12-21(13-11-20)33-26(35)18-6-8-19(9-7-18)31-24-14-15-29-23-5-3-2-4-22(23)24/h2-16H,1H3,(H,29,31)(H,33,35)(H3,28,30,32,34)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

SGI-1027 was used at 10-300 µM final concentration in various in vitro assays.

References:

  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.


Documents

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal 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