Free shipping on all orders over $ 500

PBIT

Cat. No. M15089
PBIT  Structure
Size Price Availability Quantity
2mg USD 55  USD55 In stock
5mg USD 98  USD98 In stock
10mg USD 155  USD155 In stock
25mg USD 335  USD335 In stock
50mg USD 555  USD555 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 241.31
Formula C14H11NOS
CAS Number 2514-30-9
Solubility (25°C) DMSO ≥ 40 mg/mL
Storage 2-8°C
Conversion of different model animals based on BSA (PMID: 27057123)
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 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.

References

[1] Tatsuhiko Ohto, et al. Small. Single-Molecule Conductance of a π-Hybridized Tripodal Anchor while Maintaining Electronic Communication

[2] Shalonda Kelly, et al. Fam Process. Principle-Based Integrative Therapy with Couples: Theory and a Case Example

[3] 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

[4] Gauri Shende, et al. Bioinformatics. PBIT: Pipeline Builder for Identification of drug Targets for infectious diseases

[5] 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

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

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 mesylate

Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM).

NCGC00244536

NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM.

  Catalog
Abmole Inhibitor Catalog




Keywords: PBIT supplier, Histone demethylases, inhibitors, activators

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.