JIB-04 (NSC-693627)

Alias: NSC-693627; NSC 693627; NSC693627; JIB-04; JIB 04; JIB04;
Cat No.:V0371 Purity: ≥98%
JIB-04 (also known as NSC693627) is anovel, potent and pan-selective inhibitor of Jumonji histone demethylase (JMJD) inhibitor with antineoplastic activity.
JIB-04 (NSC-693627) Chemical Structure CAS No.: 199596-05-9
Product category: Histone Demethylase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
100mg
250mg
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Other Forms of JIB-04 (NSC-693627):

  • JIB-04 Z-isomer
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

JIB-04 (also known as NSC693627) is a novel, potent and pan-selective inhibitor of Jumonji histone demethylase (JMJD) inhibitor with antineoplastic activity. As an epigenetic modifier, it inhibits JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D with IC50 values of 230, 340, 855, 445, 435, 1100, and 290 nM, respectively. JIB-04 inhibits cancer cell growth in vitro selectively and reduces in vivo tumor growth in H358 and A549 mouse xenograft models. It also prolongs the survival of mice with breast cancer.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Compared to HBEC and PrSC/PrEC, JIB-04 was consistently more selective for cancer and normal cells, as demonstrated by its increased sensitivity in lung and prostate cancer cell lines (IC50 as low as 10nM). Jumonji demethylase activity in cells is inhibited by JIB-04, and JIB-04's function in cells is influenced by Jumonji levels [1]. The proliferation of GB cell lines and stem cell-enriched cultures is markedly inhibited by JIB-04. JIB-04 causes H3K4 hypermethylation, controls the expression of genes involved in limiting the proliferation of cancer cells, and has the strongest inhibitory effect on KDM5A. Furthermore, JIB-04 (2500 nM) inactivates PI3K and activates the pathways involved de autophagy and apoptosis. JIB-04 and TMZ work together to destroy GB cells as well[2].
ln Vivo
JIB-04 significantly lowers the rates of cancer-related mortality in mice, extending their lifespan[1]. The mice's brains contain bioactive concentrations of JIB-04 (60, 40, and 20 mg/kg, ip). With a Hazard Ratio of 0.5, the orthotopic GB xenograft model indicates a tendency toward prolonged survival in mice treated with JIB-04[2].
Animal Protocol
Dissolved in 12.5% Cremophor EL, 12.5% DMSO, 10% DMSO 90% sesame oil (H358, i.p.); 110 mg/kg (H358, i.p.), 55 mg/kg (A549, Oral gavage); i.p. or p.o.
Mice harboring H358 xenografts or A549 xenografts
References
[1]. Wang L, et al. A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth. Nat Commun, 2013. 4: p. 2035.
[2]. Banelli B, et al. Small molecules targeting histone demethylase genes (KDMs) inhibit growth of temozolomide-resistant glioblastoma cells. Oncotarget. 2017 Apr 4
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H13CLN4
Molecular Weight
308.76
CAS #
199596-05-9
SMILES
C1=CC=CC=C1/C(/C1=CC=CC=N1)=N\NC1N=CC(Cl)=CC=1
InChi Key
YHHFKWKMXWRVTJ-OQKWZONESA-N
InChi Code
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+
Chemical Name
(E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine
Synonyms
NSC-693627; NSC 693627; NSC693627; JIB-04; JIB 04; JIB04;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 25 mg/mL (80.9 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.2388 mL 16.1938 mL 32.3876 mL
5 mM 0.6478 mL 3.2388 mL 6.4775 mL
10 mM 0.3239 mL 1.6194 mL 3.2388 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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