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SML1107

Sigma-Aldrich

SGC0946

≥98% (HPLC)

Synonym(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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100 μG
CN¥4,292.44

CN¥4,292.44

Estimated to ship onAugust 04, 2025Details

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100 μG
CN¥4,292.44

About This Item

Empirical Formula (Hill Notation):
C28H40BrN7O4
CAS Number:
1561178-17-3
Molecular Weight:
618.57
MDL number:
MFCD26523136
UNSPSC Code:
12352200
PubChem Substance ID:
329825482
NACRES:
NA.77

CN¥4,292.44

Estimated to ship onAugust 04, 2025Details

New, lower price on this item!
Request a Bulk Order

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

−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

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This Item
SAB5200775SAB5200766SAB5200764
Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Apc antibody produced in mouse clone S245-36, purified immunoglobulin

SAB5200772

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Apc antibody produced in mouse

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Hrp antibody produced in mouse clone S245-36, purified immunoglobulin

SAB5200775

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Hrp antibody produced in mouse

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Atto 594 antibody produced in mouse clone S245-36, purified immunoglobulin

SAB5200766

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Atto 594 antibody produced in mouse

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Atto 488 antibody produced in mouse clone S245-36, purified immunoglobulin

SAB5200764

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Atto 488 antibody produced in mouse

antibody form

purified immunoglobulin

antibody form

purified immunoglobulin

antibody form

purified immunoglobulin

antibody form

purified immunoglobulin

biological source

mouse

biological source

mouse

biological source

mouse

biological source

mouse

species reactivity

mouse, rat

species reactivity

rat, mouse

species reactivity

mouse, rat

species reactivity

rat, mouse

Gene Information

rat ... Cacng2(84347)

Gene Information

rat ... Cacng2(84347)

Gene Information

rat ... Cacng2(84347)

Gene Information

rat ... Cacng2(84347)

clone

S245-36, monoclonal

clone

S245-36, monoclonal

clone

S245-36, monoclonal

clone

S245-36, monoclonal

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.

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Pictograms

Skull and crossbones
GHS06

Signal Word

Danger

Hazard Statements

H301

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

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    Certificates of Analysis (COA)

    Lot/Batch Number
    0000414880
    0000414880
    0000251480
    0000251478
    0000241538

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    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
    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
    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
    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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    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.

    Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

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