JIB-04 (NSC693627), Jumonji Histone Demethylase Inhibitor


Catalog No. size PriceQuantity
M60132-2D 10 mM in DMSO (0.648 mL) $119
M60132-2S 2mg solid $119
M60132-10S 10mg solid $476

Description

Product Information
Molecular Weight: 308.76
Formula: C17H13ClN4
Purity: ≥98%
CAS#: n/a
Solubility: DMSO up to 50 mM
Chemical Name: (E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

JIB-04 (NSC693627, E-isomer) is a potent, selective and cell permeable Jumonji histone demethylase inhibitor. Unlike the other known inhibitors, JIB-04 is not a competitive inhibitor of a-ketoglutarate. It inhibits the demethylase activity of Jumonji enzymes in vitro, with IC50 ~230 nM for  JARID1A (KDM5A), ~440 nM for JMJD2A (KDM4A) and JMJD2B (KDM4B), ~340 nM for JMJD2E (KDM2E), and ~1 µM for JMJD3 (KDM6B) and JMJD2C (KDM4C). JIB-04 blocks Jumonji demethylase activity in cells and consequently inhibits cell growth, without affecting other a-ketoglutarate-dependent hydroxylases or histone-modifying enzymes, especially HDACs. JIB-04 alters transcriptional programs in cancer but not in normal cells, leading to cancer-specific cell death. Importantly, in vivo, JIB-04 lowers histone demethylase activity in tumors, reduces tumor burden and prolongs survival of mice in an aggressive breast cancer model.

 

How to Use:

 

  • In vitro:  JIB-04 was used at 1 µM final concentration in various in vitro assays.
  • In vivo: JIB-04 was administered 2–3 times weekly by IP injection at 110 mg/kg in sesame oil (H358 xenografts) or by gavage in Cremophor EL at 55 mg/kg (A549 xenografts) for 4-6 weeks.

 

 

Reference: 

  • 1. Wang L, et al. A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth. (2013) Nat Commun. 4:2035

 

 


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