Product Name :
JIB-04 (NSC693627) — Jumonji Histone Demethylase Inhibitor
Description:
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.
CAS:
199596-05-9
Molecular Weight:
308.76
Formula:
C17H13ClN4
Chemical Name:
(E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine
Smiles :
ClC1=CN=C(C=C1)N/N=C(/C1=CC=CC=N1)\C1C=CC=CC=1
InChiKey:
YHHFKWKMXWRVTJ-OQKWZONESA-N
InChi :
InChI=1S/C17H13ClN4/c18-14-9-10-16(20-12-14)21-22-17(13-6-2-1-3-7-13)15-8-4-5-11-19-15/h1-12H,(H,20,21)/b22-17+
Purity:
≥98% (or refer to the Certificate of Analysis)
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.{{Anti-Mouse CD44 Antibody} MedChemExpress|{Anti-Mouse CD44 Antibody} Technical Information|{Anti-Mouse CD44 Antibody} In Vivo|{Anti-Mouse CD44 Antibody} supplier|{Anti-Mouse CD44 Antibody} Cancer}
Shelf Life:
≥12 months if stored properly.{{Neratinib} web|{Neratinib} EGFR|{Neratinib} Purity & Documentation|{Neratinib} In stock|{Neratinib} custom synthesis|{Neratinib} Epigenetic Reader Domain}
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:24982871
Additional information:
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.|Product information|CAS Number: 199596-05-9|Molecular Weight: 308.76|Formula: C17H13ClN4|Chemical Name: (E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine|Smiles: ClC1=CN=C(C=C1)N/N=C(/C1=CC=CC=N1)\C1C=CC=CC=1|InChiKey: YHHFKWKMXWRVTJ-OQKWZONESA-N|InChi: InChI=1S/C17H13ClN4/c18-14-9-10-16(20-12-14)21-22-17(13-6-2-1-3-7-13)15-8-4-5-11-19-15/h1-12H,(H,20,21)/b22-17+|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:|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.|References:|Wang L, et al. A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth. (2013) Nat Commun. 4:2035Products are for research use only. Not for human use.|Documents||
