2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one

ChemicalBook > CAS DataBase List > 2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one

2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one

Product Name: 2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one
CAS No.: 2514-30-9
Chemical Name: 2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one
Synonyms: PBIT;CS-1495;PBIT, >=98%;PBIT >=98% (HPLC);JUMONJI HDM INHIBITOR;2-p-Tolyl-1,2-benzisothiazolin-3-one;2-(p-Tolyl)benzo[d]isothiazol-3(2H)-one;2-(4-methylphenyl)-1,2-benzothiazol-3-one;Histone Demethylase,Inhibitor,PBIT,inhibit;1,2-Benzisothiazol-3(2H)-one, 2-(4-methylphenyl)-
CBNumber: CB92681578
Molecular Formula: C14H11NOS
Formula Weight: 241.31
MOL File: 2514-30-9.mol

Less

2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one Property

Melting point:: 136.7-137.1 °C(Solv: benzene (71-43-2); hexane (110-54-3))
Boiling point:: 418.2±38.0 °C(Predicted)
Density: 1.297±0.06 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: DMSO: soluble10mg/mL, clear (warmed)
form: powder
pka: -0.03±0.20(Predicted)
color: white to beige
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.

Less

Safety

WGK Germany: 3

Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P501Dispose of contents/container to..…

Less

N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1058
Product name: PBIT
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $118
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML1058
Product name: PBIT
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $476
Updated: 2024/03/01

Cayman Chemical

Product number: 16272
Product name: PBIT
Purity: ≥98%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 16272
Product name: PBIT
Purity: ≥98%
Packaging: 5mg
Price: $90
Updated: 2024/03/01

Cayman Chemical

Product number: 16272
Product name: PBIT
Purity: ≥98%
Packaging: 10mg
Price: $161
Updated: 2024/03/01

Less

2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one Chemical Properties,Usage,Production

Description

Jumonji AT-rich interactive domain 1 (JARID1) demethylases mediate the removal of methyl groups from trimethylated lysine 4 on histone 3 (H3K4me3). PBIT is a reversible, cell-permeable inhibitor of JARID1 family demethylases (IC₅₀s = 6, 3, 4.9, and 28 μM for JARID1A, JARID1B, JARID1C, and JARID1D, respectively). It does not significantly affect the activity of UTX and JMJD3 demethylases. It increases trimethylation of H3K4 in HeLa cells and blocks the proliferation of tumor cells expressing high levels of JARID1B.

Biological Activity

PBIT is a specific Jumonji/AT-rich interaction domain 1 (JARID1) inhibitor. PBIT inhibits the JARID1B (KDM5B or PLU1) histone demethylase with an IC50 value of approximately 3 μM. PBIT also inhibits JARID1A and JARID1C with IC50 of 6 μM and 4.9 μM, respectively.

Biochem/physiol Actions

PBIT is a potent inhibitor of JARID1B (KDM5B) histone lysine demethylase that inhibits removal of H3K4me3 in UACC-812 cells. PBIT inhibits proliferation of cells overexpressing JARID1B. PBIT is selective for JARID1 enzymes and does not inhibit demethylases UTX or JMJD3.

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.

Enzyme inhibitor

This JARID1 Histone Demethylase inhibitor (FW = 241.31 g/mol; CAS 2514-30-9; Soluble to 100 mM in DMSO), also named 2-(4-methylphenyl)- 1,2-benzisothiazol-3(2H)-one, targets the Jumonji AT-Rich Interactive Domain 1, with respective IC50 values of 3, 4.9 and 6 μM for JARID1B, JARID1A and JARID1C. The enzymes responsible for the demethylation of trimethylated lysine 4 in histone H3 (H3K4me3) are the Jumonji AT-rich interactive domain 1 (JARID1) or lysine demethylase-5 (KDM5) family of lysine demethylases. This family consists of JARID1A (also known as KDM5A or RBP2), JARID1B (also known as KDM5B or PLU1), JARID1C (also known as KDM5C or SMCX), and JARID1D (also known as KDM5D or SMCY) in mammals. Like other JmjC domain-containing demethylases, JARID1 enzymes catalyze histon demethylation in a Fe(II) and α-ketoglutarate (α-KG)-dependent reaction. Oxidative decarboxylation of α-KG results in an unstable hydroxylated methyl-lysine intermediate. Release of the hydroxyl and methyl groups as formaldehyde from this intermediate results in demethylation. JARID1 demethylases have been linked to human diseases such as cancer and X-linked mental retardation. Both JARID1A and JARID1B are potential oncoproteins, and both are overexpressed in a variety of cancers. Increased expression of JARID1A promotes a more stem-like phenotype and enhanced resistance to anticancer agents. PBIT was identified by high-throughput screening (using biotinylated H3K4me3 peptide substrate) of agents that are selective for JARID1 over UTX and JMJD3. PBIT increases levels of methylated H3K4 in JARIDB1-transfected HeLa cells and MCF7 cells. (JARID1A and JARID1B knock-out mice are viable, suggesting that inhibition of JARID1A or JARID1B has minimal effects on normal cells in vivo. ) PBIT also inhibits proliferation of breast cancer cell lines expressing high levels of JARIDB1.

IC 50

6, 3, 4.9, and 28 μm for jarid1a, jarid1b, jarid1c, and jarid1d, respectively

References

1) Sayegh?et al.?(2013),?Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen; J. Biol. Chem.,?288?9408

2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one Preparation Products And Raw materials

Raw materials

Preparation Products

Less

2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one Suppliers

China 54 India 1 United Kingdom 1 United States 10 Global 66

EnliPharma Technology Co., Ltd

Tel: 0551-66399836 18955197623
Email: sales@enlipharma.com
Country: China
ProdList: 1874
Advantage: 55

AdooQ Bioscience CHINA

Tel: 025-58849295 18951903616;
Fax: 025-68650336
Email: info@adooq.cn
Country: China
ProdList: 2989
Advantage: 60

Sigma-Aldrich

Tel: 021-61415566 800-8193336
Email: orderCN@merckgroup.com
Country: China
ProdList: 51471
Advantage: 80

D&C Chemicals

Tel: +86-21-58447131
Fax: +86-21-61642470
Email: 1724405207@qq.com
Country: China
ProdList: 472
Advantage: 55

Lancrix Chemicals

Tel: 86-21-50817262
Fax: 86-21-57712035
Email: sales@lancrix.com
Country: China
ProdList: 1503
Advantage: 55

Shanghai SuperLan Chemcial Technique Centre

Tel: 021-2022843681 15618226720
Fax: +86-21-51601218
Email: chaolaichem@foxmail.com
Country: China
ProdList: 9038
Advantage: 58

MQ (shanghai) Pharmaceuticals Co., Ltd.

Tel: 13761635123
Fax: 1014988033@qq
Email: 1014988033@qq.com
Country: China
ProdList: 4986
Advantage: 55

Aikon International Limited

Tel: 025-58851090 13611564524
Fax: (6)02557626880
Email: lwan@aikonchem.com
Country: China
ProdList: 15952
Advantage: 58

Career Henan Chemica Co

Tel: +86-0371-86658258 15093356674;
Fax: 0371-86658258
Email: laboratory@coreychem.com
Country: China
ProdList: 30255
Advantage: 58

DC Chemicals

Tel: 021-58447131 13564518121
Email: sales@dcchemicals.com
Country: China
ProdList: 9414
Advantage: 58

Changzhou Chenhong Biotechnology Co., Ltd.

Tel: 0519-85788828 13775037613
Email: sales@chemrenpharm.com
Country: China
ProdList: 3574
Advantage: 58

Absin Bioscience Inc.

Tel: 021-38015121 15000105423
Email: chenjw@absin.cn
Country: China
ProdList: 24734
Advantage: 58

Energy Chemical

Tel: 021-58432009 400-005-6266
Fax: 021-58436166
Email: marketing1@energy-chemical.com
Country: China
ProdList: 44843
Advantage: 58

MedBioPharmaceutical Technology Inc

Tel: 021-69568360 18916172912
Email: order@med-bio.cn
Country: China
ProdList: 8141
Advantage: 58

Beijing Jin Ming Biotechnology Co., Ltd.

Tel: 010-60605840
Email: psaitong@jm-bio.com
Country: China
ProdList: 29778
Advantage: 58

Bide Pharmatech Ltd.

Tel: 400-1647117 15221909166
Email: product02@bidepharm.com
Country: China
ProdList: 63720
Advantage: 58

Kaifeng Mingren Pharmaceutical Co.,LTD

Tel: 0371-65741762
Fax: QQ：2860768577
Email: sales@hasunny.com
Country: China
ProdList: 2380
Advantage: 58

InvivoChem

Tel: 13549236410
Email: sales@invivochem.cn
Country: China
ProdList: 6713
Advantage: 58

TargetMol Chemicals Inc.

Tel: 4008200310
Email: marketing@tsbiochem.com
Country: China
ProdList: 24018
Advantage: 58

Shaanxi Cuikang Pharmaceutical Technology Co., Ltd

Tel: 18049165724 13186333400
Email: cuichengbio@163.com
Country: China
ProdList: 2605
Advantage: 58

Henan Dowon Chemical Technology Co., Ltd.

Tel: 16603857855
Email: 779113375@qq.com
Country: China
ProdList: 6643
Advantage: 58

Nantong QuanYi Biotechnology Co., Ltd

Tel: 0513-66337626 18051384581
Email: sales@chemhifuture.com
Country: China
ProdList: 4191
Advantage: 58

Shanghai Yifei Biotechnology Co. , Ltd.

Tel: 021-65675885 18964387627
Email: customer_service@efebio.com
Country: China
ProdList: 8740
Advantage: 58

Sichuan Yiyan Pharmaceutical Research

Tel: 19949968070
Email: 2904199885@qq.com
Country: China
ProdList: 917
Advantage: 58

Shanghai Aladdin Biochemical Technology Co.,Ltd.

Tel: +86-18521732826
Email: market@aladdin-e.com
Country: China
ProdList: 48467
Advantage: 58

RD International Technology Co., Limited

Tel: 18024082417
Email: market@ubiochem.com
Country: China
ProdList: 9180
Advantage: 58

ATK CHEMICAL COMPANY LIMITED

Tel: +undefined-21-51877795
Fax: +86 21 5161 9052/ 5187 7796
Email: ivan@atkchemical.com
Country: China
ProdList: 32686
Advantage: 60

Shaanxi Cuikang Pharmaceutical Technology Co., Ltd

Tel: +86-19164747840 +86-13119157289
Email: 13119157289@163.com
Country: China
ProdList: 2971
Advantage: 58

ShenZhen Trendseen Biological Technology Co.,Ltd.

Tel: 13417589054
Email: trendseenbio@gmail.com
Country: China
ProdList: 11681
Advantage: 58

Wuhan Han Sheng New Material Technology Co.，Ltd

Tel: +8617798174412
Email: admin01@hsnm.com.cn
Country: China
ProdList: 2118
Advantage: 58

Shanghai Hao Zhun Biological Technology Co., Ltd.

Tel: --
Fax: --
Email: info@zzsrm.com
Country: CHINA
ProdList: 6846
Advantage: 58

Shanghai Yuqi Biological Technology Co., Ltd.

Tel: --
Fax: --
Email: 847627550@qq.com
Country: CHINA
ProdList: 6087
Advantage: 58

Beijing Huaxia Ocean Technology Co., Ltd.

Tel: --
Fax: --
Email: huaxiabio@163.com
Country: CHINA
ProdList: 6122
Advantage: 58

Guangzhou Yuansheng Pharmaceutical Technology Co., Ltd.

Tel: --
Fax: --
Email: stemrd@curegenix.com
Country: CHINA
ProdList: 18
Advantage: 58

Qingdao Jieshikang Biotechnology Co., Ltd.

Tel: --
Fax: --
Email: jskangchina@163.com
Country: CHINA
ProdList: 4012
Advantage: 58

Shanghai Minmin Biotechnology Co., Ltd.

Tel: --
Fax: --
Email: 1914109725@qq.com
Country: CHINA
ProdList: 6530
Advantage: 58

Shanghai Weiwei Biological Technology Co., Ltd.

Tel: --
Fax: --
Email: sales@wheybio.com
Country: CHINA
ProdList: 4398
Advantage: 58

Beijing Fubo Biotechnology Co., Ltd.

Tel: --
Fax: --
Email: info@f-biology.com
Country: CHINA
ProdList: 6039
Advantage: 58

Shanghai Boyi Biotechnology Co., Ltd.

Tel: --
Fax: --
Email: 15800446246@163.com
Country: CHINA
ProdList: 5417
Advantage: 58

Shanghai Yaoyun Biological Technology Co., Ltd.

Tel: --
Fax: --
Email: 912529879@qq.com
Country: CHINA
ProdList: 6852
Advantage: 58

Beijing Bolide Biotechnology Co., Ltd.

Tel: --
Fax: --
Email: 1985563437@qq.com
Country: CHINA
ProdList: 6172
Advantage: 58

Morning Student Science and Technology (Guangzhou) Co., Ltd.

Tel: --
Fax: --
Email: chenxue_gz@163.com
Country: CHINA
ProdList: 6618
Advantage: 58

Shanghai Jijin Chemical Technology Co., Ltd.

Tel: --
Fax: --
Email: jijinhuaxue@sina.com
Country: CHINA
ProdList: 6617
Advantage: 58

Beijing Baiao Innovation Technology Co., Ltd.

Tel: --
Fax: --
Email: 3007606172@qq.com
Country: CHINA
ProdList: 6005
Advantage: 58

Boao Pike

Tel: --
Fax: --
Email: lyn@biopike.com.cn
Country: CHINA
ProdList: 6629
Advantage: 58

Shanghai Hao Biological Technology Co., Ltd.

Tel: --
Fax: --
Email: shxiyuanbio@163.com
Country: CHINA
ProdList: 6921
Advantage: 58

Xiamen Huijia Biological Technology Co., Ltd.

Tel: --
Fax: --
Country: CHINA
ProdList: 6979
Advantage: 58

Xiamen Research Biotechnology Co., Ltd.

Tel: --
Fax: --
Email: 1562893815@qq.com
Country: CHINA
ProdList: 6942
Advantage: 58

Wuhan Boot Biotechnology Co., Ltd.

Tel: --
Fax: --
Country: CHINA
ProdList: 6829
Advantage: 58

Beijing Bai Ao Si Biotechnology Co., Ltd.

Tel: --
Fax: --
Email: yangmei@bioneeds.net
Country: CHINA
ProdList: 6999
Advantage: 58

2514-30-9, 2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-oneRelated Search:

Sunitinib Malate Troglitazone ZM 447439 TYRPHOSTIN AG 1296 2-Phenylindole

2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one

2-(4-Methylphenyl)-2,3-dihydrobenzisothiazol-3-one

2-p-Tolyl-1,2-benzisothiazolin-3-one

PBIT

PBIT, >=98%

JUMONJI HDM INHIBITOR

CS-1495

2-(4-methylphenyl)-1,2-benzothiazol-3-one

1,2-Benzisothiazol-3(2H)-one, 2-(4-methylphenyl)-

PBIT >=98% (HPLC)

2-(p-Tolyl)benzo[d]isothiazol-3(2H)-one

Histone Demethylase,Inhibitor,PBIT,inhibit

2514-30-9