UNC 1999

한글명:UNC 1999

카스 번호1431612-23-5

상품명:UNC 1999

CBNumberCB02666695

분자식C33H43N7O2

포뮬러 무게569.74

MOL 파일1431612-23-5.mol

화학적 성질

끓는 점	804.7±65.0 °C(Predicted)
밀도	1.23±0.1 g/cm3(Predicted)
저장 조건	2-8°C
용해도	DMSO: 용해성15mg/mL, 투명
산도 계수 (pKa)	11.84±0.10(Predicted)
물리적 상태	가루
색상	흰색에서 베이지색
안정성	제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO의 솔루션은 -20°에서 최대 3개월 동안 보관할 수 있습니다.
InChIKey	DPJNKUOXBZSZAI-UHFFFAOYSA-N
CAS 데이터베이스	1431612-23-5

위험 및 안전 성명

위험품 표기

위험 카페고리 넘버

WGK 독일

NFPA 704:

	0
2		0

그림문자(GHS)

UNC 1999 화학적 특성, 용도, 생산

용도
The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. UNC1999 is a cell-permeable EZH2 inhibitor (IC50 = 2 nM) that is 22-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases. UNC1999 has been shown to inhibit H3K27 methylation in MCF10A cells with an IC50 value of 124 nM.[Cayman Chemical]
Biochem/physiol Actions
The polycomb repressive complex 2 (PRC2), which represses gene expression through methylation of histone H3 on lysine 27 (H3K27), contains either EZH1 or EZH2 as its catalytic subunit, with EZH1 being found in both dividing and non-dividing cells, whereas EZH2 is only found in actively dividing cells. UNC1999 is an orally bioavaliable selective inhibitor of both EZH2 and EZH1 lysine methyltransferases with IC50 < 10 nM for EZH2 and 45 nM for EZH1. UNC1999 potently inhibited both wild-type and mutant Y641N EZH2 methyltransferase activity with less than a 5-fold difference in potency, and selectively killed diffused large B cell lymphoma (DLBCL) cells bearing Y641 point mutations. It was selective for EZH2 and EZH1 over 15 other lysine, arginine and DNA methyltransferases. UNC1999 is competitive with the cofactor S-adenosylmethionine (SAM) and non-competitive with the peptide substrate. Because it inhibits both EZH2 and EZH1, UNC1999 has potential advantages over EZH2 selective inhibitors in the disease settings where both PRC2 – EZH2 and PRC2 – EZH1 contribute to the methylation of H3K27. For full characterization details, please visit the UNC1999 probe summary on the Structural Genomics Consortium (SGC) website.UNC2400 is the negative control for the active probe, UNC1999. To request a sample of the negative control from the SGC, click here.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

UNC 1999 공급 업체

Send Inquriy