| Identification | Back Directory | [Name]
SI-2 | [CAS]
380537-35-9 | [Synonyms]
SI-2
(E)-SI-2
(E)SI2,(E) SI 2
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)- | [Molecular Formula]
C15H15N5 | [MDL Number]
MFCD30537542 | [MOL File]
380537-35-9.mol | [Molecular Weight]
265.313 |
| Chemical Properties | Back Directory | [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). | [form ]
solid | [pka]
11.05±0.70(Predicted) | [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. |
| Hazard Information | Back Directory | [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. | [storage]
Store at -20°C | [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 |
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