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Submit ReviewJIB 04
Description: Pan Jumonji inhibitor; active in vivo
Chemical Name: 5-Chloro-2-[(E)-2-[phenyl(pyridin-2-yl)methylidene]hydrazin-1-yl]pyridine
Purity: ≥99% (HPLC)
Biological Activity for JIB 04
JIB 04 is a pan Jumonji histone demethylase inhibitor (IC50 values are 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C respectively). Exhibits negligible activity at PHD2 and TET1. Selectively blocks cancer cell growth in vitro and diminishes tumor growth in H358 and A549 mouse xenograft models in vivo. Prolongs survival in a mouse model of breast cancer.
Compound Libraries for JIB 04
JIB 04 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for JIB 04
| M. Wt | 308.76 |
| Formula | C17H13ClN4 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 199596-05-9 |
| PubChem ID | 6519698 |
| InChI Key | YHHFKWKMXWRVTJ-OQKWZONESA-N |
| Smiles | ClC(C=C3)=CN=C3N/N=C(C2=CC=CC=C2)/C1=CC=CC=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for JIB 04
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 30.88 | 100 |
Preparing Stock Solutions for JIB 04
The following data is based on the product molecular weight 308.76. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.24 mL | 16.19 mL | 32.39 mL |
| 5 mM | 0.65 mL | 3.24 mL | 6.48 mL |
| 10 mM | 0.32 mL | 1.62 mL | 3.24 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.65 mL |
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Product Datasheets for JIB 04
References for JIB 04
References are publications that support the biological activity of the product.
Wang et al (2013) A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth. Nat. Commun. 4 2035 PMID: 23792809
Grunicke and Hofmann (1997) Azinyl and diazinyl hydrazones derived from aryl N-heteroaryl ketones: synthesis and antiproliferative activity. J. Med. Chem. 40 4420 PMID: 9435912
If you know of a relevant reference for JIB 04, please let us know.
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Keywords: JIB 04, JIB 04 supplier, JIB04, histone, demethylases, inhibits, inhibitors, JMJ, JARID1A, JMJD2A, JMJD2B, JMJD2C, JMJD2E, JMJD3, pan, selective, antiproliferative, Histone, Demethylases, 4972, Tocris Bioscience
7 Citations for JIB 04
Citations are publications that use Tocris products. Selected citations for JIB 04 include:
Poulard et al (2018) Increasing G9a automethylation sensitizes B acute lymphoblastic leukemia cells to glucocorticoid-induced death. Cell Death Dis 9 1038 PMID: 30305606
Rowbotham et al (2018) H3K9 methyltransferases and demethylases control lung tumor-propagating cells and lung cancer progression. Nat Commun 9 4559 PMID: 30455465
Jin Kyung et al (2021) BIX01294 inhibits EGFR signaling in EGFR-mutant lung adenocarcinoma cells through a BCKDHA-mediated reduction in the EGFR level. Exp Mol Med 53 1877-1887 PMID: 34876693
Jan E et al (2021) Inhibitor of growth protein 3 epigenetically silences endogenous retroviral elements and prevents innate immune activation. Nucleic Acids Res 49 12706-12715 PMID: 34791430
Lee et al (2016) Signalling couples hair follicle stem cell quiescence with reduced histone H3 K4/K9/K27me3 for proper tissue homeostasis. Nat Commun 7 11278 PMID: 27080563
Aiko et al (2020) Histone H3 K4/9/27 Trimethylation Levels Affect Wound Healing and Stem Cell Dynamics in Adult Skin. Stem Cell Reports 14 34-48 PMID: 31866458
Jorge et al (2020) Heterochromatin-Driven Nuclear Softening Protects the Genome against Mechanical Stress-Induced Damage. Cell 181 800-817.e22 PMID: 32302590
Do you know of a great paper that uses JIB 04 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.