1. Epigenetics
  2. Histone Demethylase
  3. PBIT

PBIT 

Cat. No.: HY-101451 Purity: 98.30%
Handling Instructions

PBIT est un inhibiteur spécifique des enzymes du domaine interactif 1 riche en Jumonji AT (JARID1). PBIT inhibe JARID1B (KDM5B ou PLU1) histone déméthylase avec une 50 de environ 3 μM. PBIT inhibe également les JARID1A et JARID1C avec des IC50s de 6 μM et 4,9 μM, respectivement.

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 IC50s of 6 μM and 4.9 μM, respectively.

For research use only. We do not sell to patients.

PBIT Chemical Structure

PBIT Chemical Structure

CAS No. : 2514-30-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 64 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 220 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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 IC50s of 6 μM and 4.9 μM, respectively[1].

IC50 & Target

IC50: 3 μM (JARID1B), 6 μM (JARID1A), 4.9 μM (JARID1C)[1]

In Vitro

PBIT inhibits proliferation of cells expressing higher levels of JARID1B. PBIT (1-10 μM for UACC-812 cells, 2.5-10μM for MCF7 and MCF10A cells; 72 hours) inhibits cell proliferation in a JARID1B level-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Human breast cancer cell lines (UACC-812 and MCF7) and human mammary epithelial cells (MCF10A)
Concentration: 1, 3, and 10 μM for UACC-812 cells; 2.5, 5, and 10 μM for MCF7 and MCF10A cells
Incubation Time: 72 hours
Result: Inhibited cell proliferation in a JARID1B level-dependent manner. 10 μM killed most of the UACC-812 cells, but showed minimal toxicity to MCF7 cells and MCF10A cells.
Molecular Weight

241.31

Formula

C₁₄H₁₁NOS

CAS No.

2514-30-9

SMILES

O=C1N(C2=CC=C(C)C=C2)SC3=C1C=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (414.40 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1440 mL 20.7202 mL 41.4405 mL
5 mM 0.8288 mL 4.1440 mL 8.2881 mL
10 mM 0.4144 mL 2.0720 mL 4.1440 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.36 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.30%

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Keywords:

PBITHistone DemethylaseInhibitorinhibitorinhibit

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PBIT
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HY-101451
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