JIB-04
Synonym(s):(E)-N-(5-Chloro-pyridin-2-yl)-N′-(phenyl-pyridin-2-yl-methylene)-hydrazine
- CAS NO.:199596-05-9
- Empirical Formula: C17H13ClN4
- Molecular Weight: 308.76
- MDL number: MFCD26936344
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is JIB-04?
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
The Uses of JIB-04
JIB-04 is a specific inhibitor of Jumonji demethylases.
The Uses of JIB-04
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.
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
Properties of JIB-04
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. |
Safety information for JIB-04
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H320:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for JIB-04
InChIKey | YHHFKWKMXWRVTJ-OQKWZONESA-N |
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