PBIT (Synonyms: 2-p-tolyl-1,2-Benzisothiazolin-3-one) |
رقم الكتالوجGC15301
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PBIT هو مثبط محدد لأنزيمات Jumonji AT-rich Interactive Domain 1 (JARID1)يثبط PBIT JARID1B (KDM5B أو PLU1) demethylase هيستون مع IC بحوالي 3 ميكرومتريمنع PBIT أيضًا JARID1A و JARID1C مع IC50s من 6 ميكرومتر و 4.9 ميكرومتر ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2514-30-9
Sample solution is provided at 25 µL, 10mM.
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IC50: 6, 3, 4.9, and 28 μM for JARID1A, JARID1B, JARID1C, and JARID1D, respectively
PBIT is a JARID1 family demethylases inhibitor.
JARID1B (also known as KDM5B or PLU1), a member of the JARID1 family of histone lysine demethylases, is identified for the demethylation of trimethylated lysine 27 in histone H3 that is a mark for actively transcribed genes. JARID1B is overexpressed in several cancers, such as prostate cancer, breast cancer, and lung cancer. Additionally, JARID1B is reported for mammary tumor formation in syngeneic or xenograft mouse models and JARID1B-expressing melanoma cells are related with increased self-renewal character.
In vitro: In previous study, PBIT was identified as JmjC histone demethylase inhibitor, which inhibited JARID1B with an in vitro IC50 of about 3 μM. Consistent with its inhibitory effect on JARID1B, PBIT treatment was able to inhibit the removal of H3K4me3 by JARID1B in cells. In addition, PBIT could inhibit the proliferation of cells expressing higher levels of JARID1B. These results suggested that PBIT could be regarded as a lead compound that could be further optimized for cancer therapy [1].
In vivo: Currently, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] J. Sayegh, J. Cao, M. R. Zou, et al. Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen. The Journal of Biological Chemisty 288(13), 9408-9417 (2013).
| Cas No. | 2514-30-9 | SDF | |
| المرادفات | 2-p-tolyl-1,2-Benzisothiazolin-3-one | ||
| Chemical Name | 2-(4-methylphenyl)-1,2-benzisothiazol-3(2H)-one | ||
| Canonical SMILES | O=C1C2=CC=CC=C2SN1C3=CC=C(C)C=C3 | ||
| Formula | C14H11NOS | M.Wt | 241.3 |
| الذوبان | ≤1mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1442 mL | 20.7211 mL | 41.4422 mL |
| 5 mM | 828.8 μL | 4.1442 mL | 8.2884 mL |
| 10 mM | 414.4 μL | 2.0721 mL | 4.1442 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)