PBIT
Based on 3 publication(s) in Google Scholar
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.
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- Pureza: 99.13%
- No. CAS: 2514-30-9
- Fòrmula: C14H11NOS
- Peso molecular:241.31
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PBIT
More
Actividad biológica
Descripciòn
IC50 & Target
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KDM5 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero C1008 | CC50 |
19.95 μM
Compound: 1.2
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Cytotoxicity against monkey Vero C1008 cells after 72 hrs by MTT assay
Cytotoxicity against monkey Vero C1008 cells after 72 hrs by MTT assay
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[PMID: 28159413] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human breast cancer cell lines (UACC-812 and MCF7) and human mammary epithelial cells (MCF10A)
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Concentration:1, 3, and 10 μM for UACC-812 cells; 2.5, 5, and 10 μM for MCF7 and MCF10A cells
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Incubation Time:72 hours
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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.
Chemical Information
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No. CAS 2514-30-9
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Appearance Solid
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Peso molecular 241.31
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Fòrmula C14H11NOS
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Color Off-white to brown
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SMILES
O=C1N(C2=CC=C(C)C=C2)SC3=C1C=CC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Clin Exp Med
Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]2025 Nov 25;26(1):33. PMID: 41286164 -
RNA
Histone lysine demethylase KDM5B facilitates proliferation and suppresses apoptosis in human acute myeloid leukemia cells through the miR-140-3p/BCL2 axis. [Abstract]2024 Mar 18;30(4):435-447. PMID: 38296629 -
Cytokine
Inhibition of KDM5B participates in immune microenvironment remodeling in pancreatic cancer by inducing STING expression. [Abstract]2024 Mar:175:156451. PMID: 38163400
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (207.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (10.36 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.1440 mL | 20.7202 mL | 41.4405 mL | 103.6012 mL |
| 5 mM | 0.8288 mL | 4.1440 mL | 8.2881 mL | 20.7202 mL | |
| 10 mM | 0.4144 mL | 2.0720 mL | 4.1440 mL | 10.3601 mL | |
| 15 mM | 0.2763 mL | 1.3813 mL | 2.7627 mL | 6.9067 mL | |
| 20 mM | 0.2072 mL | 1.0360 mL | 2.0720 mL | 5.1801 mL | |
| 25 mM | 0.1658 mL | 0.8288 mL | 1.6576 mL | 4.1440 mL | |
| 30 mM | 0.1381 mL | 0.6907 mL | 1.3813 mL | 3.4534 mL | |
| 40 mM | 0.1036 mL | 0.5180 mL | 1.0360 mL | 2.5900 mL | |
| 50 mM | 0.0829 mL | 0.4144 mL | 0.8288 mL | 2.0720 mL | |
| 60 mM | 0.0691 mL | 0.3453 mL | 0.6907 mL | 1.7267 mL | |
| 80 mM | 0.0518 mL | 0.2590 mL | 0.5180 mL | 1.2950 mL | |
| 100 mM | 0.0414 mL | 0.2072 mL | 0.4144 mL | 1.0360 mL |
PBIT Related Classifications
HY-101451 Related Classifications
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