PBIT
(Synonyms: 2-p-tolyl-1,2-Benzisothiazolin-3-one) 目录号 : GC15301
An inhibitor of JARID1 family demethylases
Cas No.:2514-30-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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 | |
| 别名 | 2-p-tolyl-1,2-Benzisothiazolin-3-one | ||
| 化学名 | 2-(4-methylphenyl)-1,2-benzisothiazol-3(2H)-one | ||
| Canonical SMILES | O=C1C2=CC=CC=C2SN1C3=CC=C(C)C=C3 | ||
| 分子式 | C14H11NOS | 分子量 | 241.3 |
| 溶解度 | ≤1mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1442 mL | 20.7211 mL | 41.4422 mL |
| 5 mM | 0.8288 mL | 4.1442 mL | 8.2884 mL |
| 10 mM | 0.4144 mL | 2.0721 mL | 4.1442 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。