SML1762
SI-2
≥98% (HPLC)
Synonym(s):
(1E)-1-(2-Pyridinyl)ethanone 1-(1-methyl-1H-benzoimidazol-2-yl)-hydrazone, (1E)-N-(1-Methyl-1H-benzoimidazol-2-yl)-N′-(1-pyridin-2-yl-ethylidene)-hydrazine
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About This Item
Empirical Formula (Hill Notation):
C15H15N5
CAS Number:
Molecular Weight:
265.31
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
Assay
≥98% (HPLC)
form
powder
color
, light yellow to dark orange
solubility
DMSO: 20 mg/mL, clear
storage temp.
2-8°C
SMILES string
C/C(C1=CC=CC=N1)=N\NC2=NC3=C(C=CC=C3)N2C
Related Categories
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.
SI-2 targets the receptor-interacting domain (RID) of steroid receptor coactivators (SRCs) and suppresses cellular transcriptional activity.
Signal Word
Warning
Hazard Statements
Precautionary Statements
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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