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Merck

SML1107

SGC0946

≥98% (HPLC)

Synonyme(s) :

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

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A propos de cet article

Formule empirique (notation de Hill) :
C28H40BrN7O4
Numéro CAS:
1561178-17-3
Poids moléculaire :
618.57
NACRES:
NA.77
PubChem Substance ID:
329825482
UNSPSC Code:
12352200
MDL number:
MFCD26523136

Principaux documents

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Nom du produit

SGC0946, ≥98% (HPLC)

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

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 key

IQCKJUKAQJINMK-HUBRGWSESA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

−20°C

Quality Level

100

Catégories apparentées

Biochem/physiol Actions

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.

Features and Benefits

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.

Other Notes

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.

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301

Hazard Classifications

Acute Tox. 3 Oral

Classe de stockage

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

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Certificats d'analyse (COA)

Lot/Batch Number
0000471696
0000471695
0000471695
0000471696
0000448255

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Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

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
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
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
Dan Liu et al.
Nature communications, 9(1), 1739-1739 (2018-05-02)
Chemoresistance is a major unmet clinical obstacle in ovarian cancer treatment. Epigenetics plays a pivotal role in regulating the malignant phenotype, and has the potential in developing therapeutically valuable targets that improve the dismal outcome of this disease. Here we
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