제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO 또는 에탄올 용액은 -20°C에서 최대 1개월 동안 보관할 수 있습니다.
안전
위험 및 안전 성명
위험 및 사전주의 사항 (GHS)
WGK 독일
3
그림문자(GHS):
신호 어:
Warning
유해·위험 문구:
암호
유해·위험 문구
위험 등급
범주
신호 어
그림 문자
P- 코드
H302
삼키면 유해함
급성 독성 물질 - 경구
구분 4
경고
P264, P270, P301+P312, P330, P501
H315
피부에 자극을 일으킴
피부부식성 또는 자극성물질
구분 2
경고
P264, P280, P302+P352, P321,P332+P313, P362
H319
눈에 심한 자극을 일으킴
심한 눈 손상 또는 자극성 물질
구분 2A
경고
P264, P280, P305+P351+P338,P337+P313P
H335
호흡 자극성을 일으킬 수 있음
특정 표적장기 독성 - 1회 노출;호흡기계 자극
구분 3
경고
예방조치문구:
P264
취급 후에는 손을 철저히 씻으시오.
P264
취급 후에는 손을 철저히 씻으시오.
P270
이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P280
보호장갑/보호의/보안경/안면보호구를 착용하시오.
P301+P312
삼켜서 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.
P302+P352
피부에 묻으면 다량의 물로 씻으시오.
P305+P351+P338
눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
P321
(…) 처치를 하시오.
P330
입을 씻어내시오.
P332+P313
피부 자극이 생기면 의학적인 조치· 조언을 구하시오.
P362
오염된 의복을 벗고 세척 후에 재사용하기
P501
...에 내용물 / 용기를 폐기 하시오.
NFPA 704
0
2
0
2–(4–메틸페닐)–1,2–벤즈이소티아졸–3(2H)-온 C화학적 특성, 용도, 생산
개요
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.
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.
효소 저해제
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.