2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one
2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one 物理性質
- 融点 :
- 136.7-137.1 °C(Solv: benzene (71-43-2); hexane (110-54-3))
- 沸点 :
- 418.2±38.0 °C(Predicted)
- 比重(密度) :
- 1.297±0.06 g/cm3(Predicted)
- 貯蔵温度 :
- 2-8°C
- 溶解性:
- DMSO：可溶10mg/mL、透明（加温）
- 酸解離定数(Pka):
- -0.03±0.20(Predicted)
- 外見 :
- 粉
- 色:
- 白からベージュ
- 安定性：:
- DMSO溶液またはエタノール溶液で-20°Cで最大1か月保存できます。
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| 絵表示（GHS） |
|
| 注意喚起語 |
|
| 危険有害性情報 |
| コード |
危険有害性情報 |
危険有害性クラス |
区分 |
注意喚起語 |
シンボル |
P コード |
| H302 |
飲み込むと有害 |
急性毒性、経口 |
4 |
警告 |
|
P264, P270, P301+P312, P330, P501 |
| H315 |
皮膚刺激 |
皮膚腐食性/刺激性 |
2 |
警告 |
|
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
強い眼刺激 |
眼に対する重篤な損傷性/眼刺激 性 |
2A |
警告 |
|
P264, P280, P305+P351+P338,P337+P313P |
| H335 |
呼吸器への刺激のおそれ |
特定標的臓器毒性、単回暴露； 気道刺激性 |
3 |
警告 |
|
|
|
| 注意書き |
| P264 |
取扱い後は皮膚をよく洗うこと。 |
| P264 |
取扱い後は手や顔をよく洗うこと。 |
| P270 |
この製品を使用する時に、飲食または喫煙をしないこ と。 |
| P280 |
保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。 |
| P301+P312 |
飲み込んだ場合：気分が悪い時は医師に連絡する こと。 |
| P302+P352 |
皮膚に付着した場合：多量の水と石鹸で洗うこと。 |
| P305+P351+P338 |
眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。 |
| P321 |
特別な処置が必要である（このラベルの．．． を見よ）。 |
| P330 |
口をすすぐこと。 |
| P332+P313 |
皮膚刺激が生じた場合：医師の診断/手当てを受けるこ と。 |
| P362 |
汚染された衣類を脱ぎ、再使用す場合には洗濯をすること。 |
| P501 |
内容物/容器を．．．に廃棄すること。 |
|
2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one 価格
もっと(7)
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01COBQM-4846 |
2-(4-Methylphenyl)-1,2-benzisothiazol-3(2h)-one |
2514-30-9 |
1g |
￥60000 |
2024-03-01 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01COBQM-4846 |
2-(4-Methylphenyl)-1,2-benzisothiazol-3(2h)-one |
2514-30-9 |
250mg |
￥129600 |
2023-06-01 |
購入 |
|
Sigma-Aldrich Japan
|
SML1058 |
≥98% (HPLC)
PBIT ≥98% (HPLC) |
2514-30-9 |
5mg |
￥19100 |
2024-03-01 |
購入 |
|
Sigma-Aldrich Japan
|
SML1058 |
≥98% (HPLC)
PBIT ≥98% (HPLC) |
2514-30-9 |
25mg |
￥76400 |
2024-03-01 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01FLC500211 |
2-(4-METHYLPHENYL)-1,2-BENZISOTHIAZOL-3(2H)-ONE |
2514-30-9 |
250mg |
￥250600 |
2021-03-23 |
購入 |
2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one 化学特性,用途語,生産方法
説明
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 (IC
50s = 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.
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.
酵素阻害剤
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.
2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one 上流と下流の製品情報
原材料
準備製品
2 - (4 - Methylphenyl) - 1,2 - benzisothiazol - 3(2H)-one 生産企業
Global( 66)Suppliers
2514-30-9()キーワード:
- 2514-30-9
- 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