PBIT is a JARID1 (Jumonji AT-Rich Interactive Domain 1) inhibitor with IC50 values of 3, 4.9 and 6 μM for JARID1B, 1A and 1C, respectively. It can increase trimethylation of H3K4 in HeLa cells and block the proliferation of tumor cells expressing high levels of JARID1B.
|Solubility (25°C)||DMSO ≥ 40 mg/mL|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
 Tatsuhiko Ohto, et al. Small. Single-Molecule Conductance of a π-Hybridized Tripodal Anchor while Maintaining Electronic Communication
 Shalonda Kelly, et al. Fam Process. Principle-Based Integrative Therapy with Couples: Theory and a Case Example
 Ni Shi, et al. J Funct Foods. Efficacy comparison of lyophilised black raspberries and combination of celecoxib and PBIT in prevention of carcinogen-induced oesophageal cancer in rats
 Gauri Shende, et al. Bioinformatics. PBIT: Pipeline Builder for Identification of drug Targets for infectious diseases
 Naveena B Janakiram, et al. Oncol Rep. Chemopreventive effects of PBI-Se, a selenium-containing analog of PBIT, on AOM-induced aberrant crypt foci in F344 rats
|Related Histone demethylases Products|
Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine-specific demethylase-1 (LSD1) with an IC50 of 0.25 nM.
TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. It is an orally administered CNS-permeable clinical candidate for the study of neurodevelopmental disorders, such as autism spectrum disorders.
|L-2-Hydroxyglutaric acid disodium
L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. L-2-Hydroxyglutaric acid disodium is also an inhibitor of mitochondrial creatine kinase (Mi-CK) with Km and Ki of 2.52 mM and 11.13 mM, respectively.
Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM).
NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM.
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