IAP

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1130 YM155 (Sepantronium Bromide) 89 mg/mL 55 mg/mL '6 mg/mL
S7597 BV-6 25 mg/mL 100 mg/mL 100 mg/mL
S5600 Flavokawain A -1 mg/mL 32 mg/mL -1 mg/mL
S7362 AZD5582 100 mg/mL -1 mg/mL -1 mg/mL
S7025 Embelin <1 mg/mL 59 mg/mL 12 mg/mL
S7009 LCL161 <1 mg/mL 100 mg/mL 20 mg/mL
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) <1 mg/mL 100 mg/mL 100 mg/mL
S7089 SM-164 <1 mg/mL 3 mg/mL '''''<1 mg/mL
S8681 ASTX660 <1 mg/mL 100 mg/mL 100 mg/mL

亜型選択性的な製品

IAP製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1130

YM155 (Sepantronium Bromide)

YM155 (Sepantronium Bromide) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.

S7597

BV-6

BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.

S5600

Flavokawain A

Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. Flavokawain A can down-regulation of antiapoptotic proteins, such as XIAP, survivin, and Bcl-xL, thereby changing the balance between apoptotic and antiapoptotic molecules and then induce cell death in tumor cells.

S7362

AZD5582

AZD5582, a novel small-molecule IAP inhibitor, binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM. AZD5582 induces apoptosis.

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.

S7009

LCL161

LCL-161, a small molecule second mitochondrial activator of caspase (SMAC) mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP).

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. Birinapant helps to induce apoptosis in latent HIV-1-infected cells. Phase 2.

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.

S2754

AT406 (SM-406)

AT406 (SM-406) 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.

S7089

SM-164

SM-164 is a potent, non-peptide, cell-permeable antagonist of XIAP that targets both the BIR2 and BIR3 domains with IC50 of 1.39 nM. SM-164 induces apoptosis and tumor regression.

S8681

ASTX660

ASTX660 is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP that inhibits the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1130

YM155 (Sepantronium Bromide)

YM155 (Sepantronium Bromide) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.

S7597

BV-6

BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.

S5600

Flavokawain A

Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. Flavokawain A can down-regulation of antiapoptotic proteins, such as XIAP, survivin, and Bcl-xL, thereby changing the balance between apoptotic and antiapoptotic molecules and then induce cell death in tumor cells.

S7362

AZD5582

AZD5582, a novel small-molecule IAP inhibitor, binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM. AZD5582 induces apoptosis.

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.

S7009

LCL161

LCL-161, a small molecule second mitochondrial activator of caspase (SMAC) mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP).

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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. Birinapant helps to induce apoptosis in latent HIV-1-infected cells. Phase 2.

2020, 30(4):1260-1270

2020, 21;31(3):107547

2020, 26

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.

2020, 21

2019, 9(9):2424-2438

2019, 26(3):331-339

S2754

AT406 (SM-406)

AT406 (SM-406) 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.

2020, 577(7788):109-114

2020, 22;11(5):391

2020, 21

S7089

SM-164

SM-164 is a potent, non-peptide, cell-permeable antagonist of XIAP that targets both the BIR2 and BIR3 domains with IC50 of 1.39 nM. SM-164 induces apoptosis and tumor regression.

S8681

ASTX660

ASTX660 is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP that inhibits the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively.