1. Protein Tyrosine Kinase/RTK Apoptosis
  2. Src Apoptosis
  3. SI-2

SI-2 (EPH 116) is an inhibitor for steroid receptor coactivator-3 (SRC-3), which reduces the transcriptional activity and protein concentration of SRC-3 in cells, exhibits cytotoxicity in cancer cell, with IC50s ranging from 3-20 nM, inhibits migration of MDA-MB-468, induces apoptosis of MDA-MB-468. SI-2 inhibits the tumor growth in mouse models, without significant toxicity for heart and other major organs (20 mg/kg).

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SI-2 Chemical Structure

SI-2 Chemical Structure

CAS No. : 223788-33-8

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Description

SI-2 (EPH 116) is an inhibitor for steroid receptor coactivator-3 (SRC-3), which reduces the transcriptional activity and protein concentration of SRC-3 in cells, exhibits cytotoxicity in cancer cell, with IC50s ranging from 3-20 nM, inhibits migration of MDA-MB-468, induces apoptosis of MDA-MB-468. SI-2 inhibits the tumor growth in mouse models, without significant toxicity for heart and other major organs (20 mg/kg)[1].

Cellular Effect
Cell Line Type Value Description References
TOV112D EC50
0.004 μM
Compound: C9
Growth inhibition of human TOV112D cells harbouring p53 R175H mutant incubated for 3 days by MTS assay
Growth inhibition of human TOV112D cells harbouring p53 R175H mutant incubated for 3 days by MTS assay
[PMID: 33538587]
Molecular Weight

265.31

Formula

C15H15N5

CAS No.
SMILES

CN1C(N/N=C(C)/C2=CC=CC=N2)=NC3=CC=CC=C13

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SI-2
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HY-101447
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