IAP

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IAP Inhibitors | Antagonists (6)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S7015 Birinapant Birinapant is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. Phase 2.
  • Cell Death Differ, 2016, 10.1038/cdd.2016.51
  • Cancer Lett, 2016, 10.1016/j.canlet.2016.02.040
  • Cell Death Dis, 2015, 6:e1767
S7010 GDC-0152 GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM and 43 nM in cell-free assays, respectively; less affinity shown to cIAP1-BIR2 and cIAP2-BIR2. Phase 1.
  • PLoS One, 2015, 10(5):e0128647
S2754 AT406 (SM-406, ARRY-334543) AT406 (SM-406, ARRY-334543) is a potent Smac mimetic and an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1.
  • Cancer Res, 2015, 10.1158/0008-5472.CAN-14-2199
  • Int J Oncol, 2016, 10.3892/ijo.2016.3525. Epub 2016 May 16
  • Biochem Biophys Res Commun, 2016, 478(1):293-9
S7025 Embelin Embelin, a quinone isolated from the Japanese Ardisia herb, is an inhibitor of X-linked inhibitor of apoptosis (XIAP) with IC50 of 4.1 μM in a cell-free assay.
S7597 BV-6 BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.
S7009 LCL161 LCL161, a SMAC mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP). Phase 2.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S7015 Birinapant <1 mg/mL 100 mg/mL 55 mg/mL
S7010 GDC-0152 3 mg/mL 99 mg/mL 99 mg/mL
S2754 AT406 (SM-406, ARRY-334543) <1 mg/mL 100 mg/mL 100 mg/mL
S7025 Embelin <1 mg/mL 59 mg/mL 12 mg/mL
S7597 BV-6 25 mg/mL 100 mg/mL 100 mg/mL
S7009 LCL161 <1 mg/mL 100 mg/mL 20 mg/mL
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