JIB-04(JIB04)|cas 199596-05-9|DC Chemicals

Cas No.:	199596-05-9
Chemical Name:	5-Chloro-N-[(E)-[phenyl(pyridin-2-yl)methylidene]amino]pyridin-2-amine
Synonyms:	5-chloro-N-[(E)-[phenyl(pyridin-2-yl)methylidene]amino]pyridin-2-amine;AC1O75RE;FD5031;NSC-693627;JIB-04, NSC 693627;QC-10233;S7281,NSC693627,;JIB-04;(E)-N-(5-Chloro-pyridin-2-yl)?-N-(phenyl-pyridin-2-yl-methylene)-hydrazine;JIB 04;JIB-04 (NSC 693627)(E);(E)-5-CHLORO-2-(2-(PHENYL(PYRIDIN-2-YL)METHYLENE)HYDRAZINYL)PYRIDINE;(E)-N-(5-Chloro-pyridin-2-yl)-N′-(phenyl-pyridin-2-yl-methylene)-hydrazine;NSC 693627;JIB-04 (E);NSC693627 (E);JIB-04 (NSC 693627);5-Chloro-2(1H)-pyridinone (2E)-(phenyl-2-pyridinylmethylene)hydrazone;JIB04;NCIChal_000041;5-Chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine;AK314648;NCI60_033523
SMILES:	ClC1=C([H])N=C(C([H])=C1[H])N([H])N=C(C1=C([H])C([H])=C([H])C([H])=N1)C1C([H])=C([H])C([H])=C([H])C=1[H]
Formula:	C₁₇H₁₃ClN₄
M.Wt:	308.7649
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
In Vivo:	JIB-04 results in a significant reduction in cancer-induced death rates in mice, prolonging survival[1]. JIB-04 (60, 40 and 20 mg/kg, i.p.) reaches bioactive concentration in the brain of the mice. The orthotopic GB xenograft model shows a trend toward longer survival in JIB-04-treated mice with an Hazard Ratio of 0.5[2].
In Vitro:	JIB-04 is consistently selective for cancer vs. normal cells, demonstrated by the higher sensitivity of lung and prostate cancer lines (with IC50 as low as 10 nM) compared to HBECs and PrSCs/PrECs. JIB-04 inhibits cellular Jumonji demethylase activity, and Jumonji levels affect JIB-04 action in cells[1]. JIB-04 significantly inhibits the proliferation of GB cell lines and stem-enriched cultures. JIB-04 exerts its maximal inhibitory activity against KDM5A, and modulates the expression of genes involved in the control of cancer cell growth and leads to hypermethylation of H3K4. Furthermore, JIB-04 (2500 nM) activates the autophagy and apoptotic pathways and inactivates PI3K. JIB-04 also cooperates with TMZ in killing GB cells[2].

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