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Chemical Structure| 2514-30-9 Chemical Structure| 2514-30-9

Structure of PBIT
CAS No.: 2514-30-9

Chemical Structure| 2514-30-9

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PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM. PBIT also inhibits JARID1A and JARID1C with IC50 values of 6 and 4.9 μM, respectively[1].

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Product Details of PBIT

CAS No. :2514-30-9
Formula : C14H11NOS
M.W : 241.31
SMILES Code : O=C1N(C2=CC=C(C)C=C2)SC3=C1C=CC=C3
MDL No. :MFCD05856231
InChI Key :KRXMYBAZKJBJAB-UHFFFAOYSA-N
Pubchem ID :935415

Safety of PBIT

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501

Related Pathways of PBIT

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HeLa cells 10 or 30 µM 24 hours PBIT treatment prevented the JARID1B overexpression-induced decrease of H3K4me3. J Biol Chem. 2013 Mar 29;288(13):9408-17
RWPE-1 cells 1–20 µM 72 hours To assess the effect of PBIT on the proliferation of RWPE-1 cells, results showed that PBIT significantly decreased the viability of RWPE-1 cells. Exp Cell Res. 2024 Apr 1;437(1):113991
LNCaP-MDV3100 cells 1–20 µM 72 hours To assess the effect of PBIT on the proliferation of LNCaP-MDV3100 cells, results showed that PBIT significantly decreased the viability of LNCaP-MDV3100 cells. Exp Cell Res. 2024 Apr 1;437(1):113991
PC-3 cells 1–20 µM 72 hours To assess the effect of PBIT on the proliferation of PC-3 cells, results showed that PBIT significantly decreased the viability of PC-3 cells. Exp Cell Res. 2024 Apr 1;437(1):113991
C4–2B cells 1–20 µM 72 hours To assess the effect of PBIT on the proliferation of C4–2B cells, results showed that PBIT significantly decreased the viability of C4–2B cells. Exp Cell Res. 2024 Apr 1;437(1):113991
LNCaP cells 1–20 µM 72 hours To assess the effect of PBIT on the proliferation of LNCaP cells, results showed that PBIT significantly decreased the viability of LNCaP cells. Exp Cell Res. 2024 Apr 1;437(1):113991
UACC-812 cells 10 µM 72 hours PBIT treatment significantly inhibited the proliferation of UACC-812 cells. J Biol Chem. 2013 Mar 29;288(13):9408-17
MCF7 cells 10 µM 72 hours PBIT treatment significantly increased global levels of H3K4me3. J Biol Chem. 2013 Mar 29;288(13):9408-17

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Male F344 rats NMBA-induced esophageal squamous cell carcinoma model Dietary administration 50 ppm Freshly prepared weekly, lasting for 35 weeks To evaluate the preventive effect of PBIT combined with celecoxib on NMBA-induced esophageal tumors, results showed that the combination significantly reduced tumor incidence and multiplicity. J Funct Foods. 2016 Dec;27:84-94

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.14mL

0.83mL

0.41mL

20.72mL

4.14mL

2.07mL

41.44mL

8.29mL

4.14mL

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