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| Product Name: | JIB-04 | | Synonyms: | JIB-04;JIB-04
(NSC 693627);JIB04/JIB-04;5-Chloro-2(1H)-pyridinone (2E)-(phenyl-2-pyridinylmethylene)hydrazone;(E)-5-CHLORO-2-(2-(PHENYL(PYRIDIN-2-YL)METHYLENE)HYDRAZINYL)PYRIDINE;5-Chloro-2-[(E)-2-[phenyl(pyridin-2-yl)methylidene]hydrazin-1-yl]pyridine;NSC 693627;5-Chloro-2(1H)-pyridinone (2E)-(phenyl-2-pyridinylmethylene)hydrazone JIB-04(NSC 693627) | | CAS: | 199596-05-9 | | MF: | C17H13ClN4 | | MW: | 308.76 | | EINECS: | | Product Categories: | Inhibitors | | Mol File: | 199596-05-9.mol |
| JIB-04 Chemical Properties |
| 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 |
| JIB-04 Usage And Synthesis |
| 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 is a specific inhibitor of Jumonji demethylases. | | 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). | | 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. | | References | 1) Wang?et al.?(2013),?A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth; Nature Commun., 4?2035 |
| JIB-04 Preparation Products And Raw materials |
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