Identification | Back Directory | [Name]
JIB-04 | [CAS]
199596-05-9 | [Synonyms]
JIB-04 CS-1447 NSC 693627 JIB-04 (E) JIB04/JIB-04 JIB-04, >=98% NSC693627 (E) JIB-04 USP/EP/BP JIB-04 >=98% (HPLC) JIB-04
(NSC 693627) JIB-04 (NSC 693627)(E) JIB-04(NSC 693627), >97% JIB-04 (NSC 693627), 199596-05-9(E) NSC693627;JIB04; JIB 04;NSC-693627;JIB-04;JIB04 (E)-5-CHLORO-2-(2-(PHENYL(PYRIDIN-2-YL)METHYLENE)HYDRAZINYL)PYRIDINE 5-Chloro-2(1H)-pyridinone (2E)-(phenyl-2-pyridinylmethylene)hydrazone 5-chloro-n-[(e)-[phenyl(pyridin-2-yl)methylidene]amino]pyridin-2-amine 5-Chloro-2-[(E)-2-[phenyl(pyridin-2-yl)methylidene]hydrazin-1-yl]pyridine Methanone, phenyl-2-pyridinyl-, 2-(5-chloro-2-pyridinyl)hydrazone, (E,E)- (E)-N-(5-Chloro-pyridin-2-yl)-N′-(phenyl-pyridin-2-yl-methylene)-hydrazine 5-Chloro-2(1H)-pyridinone (2E)-(phenyl-2-pyridinylmethylene)hydrazone JIB-04(NSC 693627) JIB-04 5-Chloro-2(1H)-pyridinone (2E)-(phenyl-2-pyridinylmethylene)hydrazone | [Molecular Formula]
C17H13ClN4 | [MDL Number]
MFCD26936344 | [MOL File]
199596-05-9.mol | [Molecular Weight]
308.76 |
Chemical Properties | Back Directory | [Boiling point ]
472.9±55.0 °C(Predicted) | [density ]
1.24±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble10mg/mL, clear | [form ]
powder | [pka]
11.00±0.10(Predicted) | [color ]
white to beige | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. | [InChIKey]
YHHFKWKMXWRVTJ-OQKWZONESA-N |
Hazard Information | Back Directory | [Description]
JIB-04 (199596-05-9) is a novel specific inhibitor of the Jumonji family of histone demethylases?in vitro, in cancer cells and in tumors?in vivo.?IC50?= 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C respectively.??Reduces tumor burden and prolongs life in a mouse model.1?Suppresses translation initiation and enhances mTOR inhibitor sensitivity.2?Inhibits the growth of temozolomide-resistant glioblastoma cells and crosses the blood brain barrier.3 | [Uses]
JIB-04 has been used in sulforhodamine B cell growth assay. It has also been used as a control to determine the inhibitory action of ML324 on KDM4A (histone lysine demethylase 4A). | [Uses]
JIB-04 is a specific inhibitor of Jumonji demethylases. | [Biochem/physiol Actions]
JIB-04 is a selective inihibitor of Jumonji demethylases without inhibiting other α-ketoglutarate-dependent hydroxylases or histone-modifying enzymes including amine oxidase LSD1 (also known as KDM1A), which demethylates histone lysines. JIB-04 is a pan-inhibitor of Jumonji demethylases with JARID1A (KDM5A) being the most sensitive (IC50=230 nM) followed by JMJD2D (IC50=290 nM) and JMJD3 (KDM6B) and JMJD2C (KDM4C) more resistant (IC50 855 and 1100 nM, respectively). JIB-04 selectively inhibited viability of several human cancer cell lines with little toxicity towards normal cells, and also diminished tumor growth in two separate xenograft mouse models. | [storage]
+4°C | [References]
1) Wang?et al.?(2013),?A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth; Nature Commun., 4?2035 |
|
|