콘텐츠로 건너뛰기
Merck
모든 사진(1)

주요 문서

SML1107

Sigma-Aldrich

SGC0946

≥98% (HPLC)

동의어(들):

1-(3-((((2R,3S,4R,5R)-5-(4-Amino-5-bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea, 5-Bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-7H-Pyrrolo[2,3-d]pyrimidin-4-amine

로그인조직 및 계약 가격 보기


About This Item

실험식(Hill 표기법):
C28H40BrN7O4
CAS Number:
Molecular Weight:
618.57
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: 20 mg/mL, clear

저장 온도

−20°C

SMILES string

BrC1=CN([C@@H]2O[C@H](CN(CCCNC(NC3=CC=C(C(C)(C)C)C=C3)=O)C(C)C)[C@@H](O)[C@H]2O)C4=C1C(N)=NC=N4

InChI

1S/C28H40BrN7O4/c1-16(2)35(12-6-11-31-27(39)34-18-9-7-17(8-10-18)28(3,4)5)14-20-22(37)23(38)26(40-20)36-13-19(29)21-24(30)32-15-33-25(21)36/h7-10,13,15-16,20,22-23,26,37-38H,6,11-12,14H2,1-5H3,(H2,30,32,33)(H2,31,34,39)/t20-,22-,23-,26-/m1/s1

InChI key

IQCKJUKAQJINMK-HUBRGWSESA-N

생화학적/생리학적 작용

SGC0946 is a potent and selective inhibitor of Histone H3-lysine79 (H3K79) methyltransferase DOT1L with an IC50 of 0.3 nM in a radioactive enzyme assay, and over 100-fold selectivity for DOT1L over other histone methyltransferases. In cell studies, SGC0946 reduces H3K79 dimethylation with an IC50 of 2.6 nM in A431 cells and 8.8 nM in MCF10A cells. SGC0946 was found to selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro model of leukemia. For full characterization details, please visit the SGC0946 probe summary on the Structural Genomics Consortium (SGC) website.

SGC0649 is the negative control for the active probe, SGC0946. 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
SGC0946 is a potent and selective inhibitor of Histone H3-lysine79 (H3K79) methyltransferase DOT1L.

특징 및 장점

SGC0946 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

기타 정보

SGC0946 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the SGC0946 probe summary on the Chemical Probes Portal website.

관련 제품

제품 번호
설명
가격

픽토그램

Skull and crossbones

신호어

Danger

유해 및 위험 성명서

Hazard Classifications

Acute Tox. 3 Oral

Storage Class Code

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


가장 최신 버전 중 하나를 선택하세요:

시험 성적서(COA)

Lot/Batch Number

적합한 버전을 찾을 수 없으신가요?

특정 버전이 필요한 경우 로트 번호나 배치 번호로 특정 인증서를 찾을 수 있습니다.

이 제품을 이미 가지고 계십니까?

문서 라이브러리에서 최근에 구매한 제품에 대한 문서를 찾아보세요.

문서 라이브러리 방문

Hao Zhang et al.
eLife, 9 (2020-10-02)
Aberrant HOXA9 expression is a hallmark of most aggressive acute leukemias, notably those with KMT2A (MLL) gene rearrangements. HOXA9 overexpression not only predicts poor diagnosis and outcome but also plays a critical role in leukemia transformation and maintenance. However, our
Julia Gobl et al.
Vaccines, 8(2) (2020-04-05)
Epigenetic mechanisms have not been characterized in ticks despite their importance as vectors of human and animal diseases worldwide. Our investigation identifies and functionally characterizes the orthologue of S-adenosylmethionine (SAM) binding methyltransferase enzyme, disruptor of telomeric silencing 1-like (DOT1L) in
Christiaan J Stavast et al.
Leukemia (2021-11-07)
MIR139 is a tumor suppressor and is commonly silenced in acute myeloid leukemia (AML). However, the tumor-suppressing activities of miR-139 and molecular mechanisms of MIR139-silencing remain largely unknown. Here, we studied the poorly prognostic MLL-AF9 fusion protein-expressing AML. We show
Giovanni Nassa et al.
Science advances, 5(2), eaav5590-eaav5590 (2019-02-19)
Breast cancer (BC) resistance to endocrine therapy results from constitutively active or aberrant estrogen receptor α (ERα) signaling, and ways to block ERα pathway in these tumors are sought after. We identified the H3K79 methyltransferase DOT1L as a novel cofactor
Kazuya Ishiguro et al.
Haematologica, 104(1), 155-165 (2018-09-02)
Epigenetic alterations play an important role in the pathogenesis in multiple myeloma, but their biological and clinical relevance is not fully understood. Here, we show that DOT1L, which catalyzes methylation of histone H3 lysine 79, is required for myeloma cell

문서

We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

관련 콘텐츠

당사는 유전자 조절 연구 분야에서 표적 식별 및 검증을 위해 전사 인자 조절인자, 염색질 변형 효소 억제제, 작용제/길항제와 같은 여러 저분자 연구 툴을 제공합니다. 이러한 연구 툴 제품군은 아래에 나와 있습니다.

자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..

고객지원팀으로 연락바랍니다.