SI-2 hydrochloride

SKU: orb1708527

Description

SI-2 hydrochloride (EPH 116 hydrochloride) is a potent and orally bioavailable small molecule inhibitor of the SRC-3 protein-protein interaction. It demonstrates high potency in vitro, with IC50 values of 3-20 nM for inducing breast cancer cell death, supporting its investigation in oncology research.

Research Area

Cardiovascular Research, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 1992052-49-9
• MW: 301.77
• Purity: 98.60% (May vary between batches)
• Formula: C₁₅H₁₆ClN₅
• SMILES: Cl.C\C(=N/Nc1nc2ccccc2n1C)c1ccccn1
• Target: Estrogen Receptor/ERR,Src,Others
• Solubility: DMSO:4.5 mg/mL (14.91 mM)

Bioactivity

• Target IC50:
  Breast cancer cell death:3-20 nM
• In Vivo:
  SI-2 causes minimal acute cardiotoxicity based on a hERG channel blocking assay and an unappreciable chronic toxicity to major organs based on histological analyses. SI-2 is a drug-like molecule and meets all of the criteria of Lipinski’s rule.
• In Vitro:
  SI-2 selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells through direct physical interactions with SRC-3. Breast cancer cell death selectively induced by SI-2 with IC50 of 3-20 nM. SI-2 (100 nM) decreases cell motility, invasion, and tumor metastasis in MDAMB-468 cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

breast cancer cell death, EPH 116 Hydrochloride, EPH 116 hydrochloride, EPH116 Hydrochloride, EPH-116 Hydrochloride, SI 2 Hydrochloride, SI2 Hydrochloride, SI-2 Hydrochloride, Src

Compound Identifiers

PubChem CID

121513909