SI-2

Product Name: SI-2
CAS No.: 380537-35-9
Chemical Name: SI-2
Synonyms: SI-2;(E)-SI-2;(E)SI2,(E) SI 2;(E)-SI-2, 10 mM in DMSO;1-(2-pyridinyl)-, 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone, (1E)-;Ethanone, 1-(2-pyridinyl)-, 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone, (1E)-
CBNumber: CB33152741
Molecular Formula: C15H15N5
Formula Weight: 265.313
MOL File: 380537-35-9.mol

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SI-2 Property

Boiling point:: 459.9±37.0 °C(Predicted)
Density: 1.22±0.1 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: Soluble in DMSO (up to 20 mg/ml).
pka: 11.05±0.70(Predicted)
form: solid
color: Pale orange
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1762
Product name: SI-2
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $107
Updated: 2023/06/20

Sigma-Aldrich

Product number: SML1762
Product name: SI-2
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $434
Updated: 2023/06/20

Cayman Chemical

Product number: 19565
Product name: SI-2
Purity: ≥98%
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 19565
Product name: SI-2
Purity: ≥98%
Packaging: 5mg
Price: $161
Updated: 2024/03/01

Cayman Chemical

Product number: 19565
Product name: SI-2
Purity: ≥98%
Packaging: 10mg
Price: $299
Updated: 2024/03/01

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SI-2 Chemical Properties,Usage,Production

Description

SI-2 (380537-35-9) is a potent inhibitor of steroid receptor coactivator-3 (SRC-3).1?It blocks MDA-MB-468 cell growth with an IC50?= 3.4 nM without effecting normal cells.1?It significantly inhibited breast cancer cell growth in an orthotopic MDA-MD-468 mouse model. Treatment of MCF-7 or triple negative MDA-MB-231 cells with SI-2 resulted in inhibition of proliferation and breast cancer stem cell (CSC) tumorsphere formation.2?CSC markers CD44+/CD24-/1o?and aldehyde dehydrogenase (ALDH) were also reduced indicating that SI-2 can selectively interfere with the TIC/CSC state in breast cancer cells.2,3

Uses

SI-2 is an inhibitor of steroid receptor coactivator-3 (SRC-3). Induces cell death in verious breast cancer cells.

Biochem/physiol Actions

SI-2 targets the receptor-interacting domain (RID) of steroid receptor coactivators (SRCs) and suppresses cellular transcriptional activity (Effec. conc. >/= 5 nM in cell-based SRC-1, SRC-2, and SRC-3 reporter assays) by downregulating SRCs protein, but not transcript level (Effec. conc. >/= 12.5 nM against SRC-3, >/= 25 nM against SRC-1 and SCR-2 in MDA-MB-468 culture). SI-2 is cytotoxic to breast cancer cultures (IC50?= 1.5 nM/BT-474, 3.4 nM/MDA-MB-468, 22 nM/MCF-7), but not to normal hepatocytes even at 500 nM concentration. SI-2 is reported to be orally available in mice and, when administered intraperitoneally (2 mg/kg b.i.d.), effectively suppress MDA-MB-468-derived tumor expansion in mice?in vivowith good pharmacokinetics (Cmax?= 30 μM,?tmax?= 0.25 h,?t1/2?= 1.0 h; 20 mg/kg i.p.) and no apparent adverse effects to the animals.

References

1) Song?et al.?(2016),?Development of potent small-molecule inhibitors to drug the undruggable steroid receptor coactivator-3; Proc. Natl. Acad. Sci. USA?113?4970 2) Rohira?et al.?(2017),?Targeting SRC Coactivators Blocks the Tumor-Initiating Capacity of Cancer Stem-like Cells; Cancer Res.?77?4293 3) Truong?et al.?(2018),?Cancer Stem Cell Phenotypes in ER+ Breast Cancer Models are Promoted by PELP/AIB1 Complexes; Mol. Cancer Res.?16?707

SI-2 Preparation Products And Raw materials

Raw materials

Preparation Products

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SI-2 Suppliers

China 24 United States 5 Global 29

Sigma-Aldrich

Tel: 021-61415566 800-8193336
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Shanghai EFE Biological Technology Co., Ltd.

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Shanghai Hongye Biotechnology Co. Ltd

Tel: 400-9205774
Email: sales@glpbio.cn
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TargetMol Chemicals Inc.

Tel: +1-781-999-5354 +1-00000000000
Email: marketing@targetmol.com
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Career Henan Chemica Co

Tel: +86-0371-86658258 +8613203830695
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DC Chemicals

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ChemeGen(Shanghai) Biotechnology Co.,Ltd.

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MedBioPharmaceutical Technology Inc

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Energy Chemical

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TargetMol Chemicals Inc.

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380537-35-9, SI-2Related Search:

Ko 143 Adapalene Cantharidin Troglitazone

SI-2

Ethanone, 1-(2-pyridinyl)-, 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone, (1E)-

1-(2-pyridinyl)-, 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone, (1E)-

(E)-SI-2

(E)SI2,(E) SI 2

(E)-SI-2, 10 mM in DMSO

380537-35-9