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JIB-04

Cat. No. M2275
JIB-04 Structure
Size Price Availability Quantity
10mg USD 100 In stock
50mg USD 300 In stock
100mg USD 400 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

JIB-04 is a potent, cell-permeable inhibitor of Jumonji histone demethylase in vitro and in vivo (IC50 values are 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C 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. JIB 04 selectively blocks cancer cell growth in vitro and diminishes tumor growth in H358 and A549 mouse xenograft models in vivo. JIB-04 induces transcriptional changes in a cancer-selective manner, including the downregulation of proliferative genes and the upregulation of the anti-proliferative/pro-apoptotic genes.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 308.76
Formula C17H13ClN4
CAS Number 199596-05-9
Purity >99%
Solubility DMSO 10 mg/mL
Storage at -20°C
References

A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth.
Wang L, et al. Nat Commun. 2013;4:2035. PMID: 23792809.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: JIB-04 supplier, Histone demethylases, inhibitors

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