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)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1130	YM155 (Sepantronium Bromide)	89 mg/mL	55 mg/mL	6 mg/mL
S5967	Berberine chloride hydrate	39 mg/mL	78 mg/mL	'<1 mg/mL
S7597	BV-6	25 mg/mL	100 mg/mL	100 mg/mL
S2271	Berberine chloride (NSC 646666)	<1 mg/mL	40 mg/mL	<1 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
S9634	Phenoxodiol (Haginin E)	<1 mg/mL	48 mg/mL	48 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 (TL32711)	<1 mg/mL	100 mg/mL	''55 mg/mL
S7010	GDC-0152	3 mg/mL	99 mg/mL	99 mg/mL
S2754	Xevinapant (AT406)	<1 mg/mL	100 mg/mL	'100 mg/mL
S7089	SM-164	<1 mg/mL	3 mg/mL	<1 mg/mL
S8681	Tolinapant (ASTX660)	<1 mg/mL	100 mg/mL	'100 mg/mL

亜型選択性的な製品

IAP製品

All (14) IAP阻害剤(9) IAP拮抗剤(5)

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.	Nat Commun, 2021, 12(1):2877 Nat Commun, 2021, 12(1):2475 J Clin Invest, 2021, 131(10)146777	MM cell lines UM9 (left panel) or U266 (right panel) were cultured in presence or absence of accessory cells prior to incubation with CTLs alone, YM155 alone or the combination. Survival of UM9 and U266 MM cells was assessed by CS-BLI. Results show % lysis of MM cells after 24 hour incubation and are depicted for three doses.
S5967^新	Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Pharmacol, 2021, 12:632201
S7597	BV-6 BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.	EMBO Rep, 2021, e52702 Oncogene, 2021, 10.1038/s41388-021-01869-4 Cancers (Basel), 2021, 13(14)3585	IEC-1 cells were transfected with Per1/2 specific siRNAs or a control siRNA. Afterward, the cells were stimulated with TNFa (0.1 ng/ml under basal conditions) in the presence or absence of BV-6 or were left untreated. Activation of caspase-8 (I) and caspases 3/7 (J ) was assayed. Data are presented as the means±SEM of at least 3 independent experiments. P≤0.05, *P≤0.01.
S2271	Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Pharmacol, 2021, 12:632201 Molecules, 2021, 26(5)1210 Biology (Basel), 2021, 10(3)250
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.	J Virol, 2021, JVI.01297-20 Life Sci Alliance, 2020, 28;3(6) pii: e202000735 EMBO J, 2019, 15;38(10):e101638
S9634	Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.	Anticancer Res, 2018, 38(10):5709-5716
S7025	Embelin Embelin (Embelic Acid, NSC 91874), 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.	Cancers (Basel), 2021, 13(14)3585 Cell Host Microbe, 2018, 24(5):689-702 Am J Pathol, 2018, 188(2):404-416	(d) Representative plots of apoptosis in Jurkat cells treated with vehicle only, BIO, CN585, Embelin (Emb), BIO plus CN585 or BIO plus CN585 plus Emb.
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).	Theranostics, 2021, 11(18):9009-9021 Cell Rep, 2021, 35(6):109112 Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X	Parental or rVCR RD cells were either left untreated (UT) or exposed to 40 μM of LCL161 in the absence or presence of PSC-833 (10 μM) for 48 h before analysis of DNA fragmentation using PI staining and flow cytometry (data shown are mean + SD, n = 3). , p < 0.05, , p < 0.01, **, p < 0.001.
S7015	Birinapant (TL32711) Birinapant (TL32711) is a SMAC mimetic antagonist, mostly to cIAP1 with K_d 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.	Sci Adv, 2021, 7(28)eabf4408 Nat Commun, 2021, 12(1):2482 EMBO Mol Med, 2021, e13466	Western blot analysis of XIAP and cIAP1 expression and PARP cleavage in H460, A549 and 34LU cells pre-treated with vorinostat or entinostat for 6h followed by the SMAC mimetic birinapant for 24h.
S7010	GDC-0152 GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with K_i 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.	Apoptosis, 2020, 21 Cell Death Dis, 2020, 11(8):680 Theranostics, 2019, 9(9):2424-2438	Inhibitor of Apoptosis Proteins (IAPs) were involved in MCP-1/IL-6 production under high dose TNF-α stimulation. A. hUC-MSCs (2x104 in 96-well plates) were pretreated for 2h with the IAP inhibitor GDC-0152 at increasing concentrations (0-1000 nM), then stimulated with TNF-α (20 ng/ml, 1.2 nM). After a further 24h, trypan blue was used to exclude cell toxicity. SN was collected and IL-6 and MCP-1 concentrations were measured by ELISA. B. hUC-MSCs(5×105 in T25 bottle) were pretreated with GDC-0152(1000nM) for 2 h, then stimulated with TNF-α (20 ng/ml, 1.2 nM). 24 hours later, protein from nucleus and cytoplasma were extracted separately and the amount of NF-kB were detected by Western blot. Data are as mean±SEM of triplicate measurements; p<0.05, p<0.01, **p<0.001 when compared to untreated cells. These experiments were repeated 3 times with the same results, using clone 69 and another TNF-α sensitive clone (clone 120003).
S2754	Xevinapant (AT406) Xevinapant (AT406, ARRY-334543, Debio1143, 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 K_i of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1.	Theranostics, 2021, 11(18):9009-9021 Cancers (Basel), 2021, 13(14)3585 Neoplasia, 2021, 23(5):539-550	G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting.
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.	Clin Epigenetics, 2021, 13(1):37 Cell Death Dis, 2021, 12(2):140 Cell Death Dis, 2018, 9(7):732
S8681	Tolinapant (ASTX660) Tolinapant (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.	Nat Commun, 2021, 12(1):2877 Nat Commun, 2021, 12(1):2475 J Clin Invest, 2021, 131(10)146777	MM cell lines UM9 (left panel) or U266 (right panel) were cultured in presence or absence of accessory cells prior to incubation with CTLs alone, YM155 alone or the combination. Survival of UM9 and U266 MM cells was assessed by CS-BLI. Results show % lysis of MM cells after 24 hour incubation and are depicted for three doses.
S5967^新	Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Pharmacol, 2021, 12:632201
S7597	BV-6 BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.	EMBO Rep, 2021, e52702 Oncogene, 2021, 10.1038/s41388-021-01869-4 Cancers (Basel), 2021, 13(14)3585	IEC-1 cells were transfected with Per1/2 specific siRNAs or a control siRNA. Afterward, the cells were stimulated with TNFa (0.1 ng/ml under basal conditions) in the presence or absence of BV-6 or were left untreated. Activation of caspase-8 (I) and caspases 3/7 (J ) was assayed. Data are presented as the means±SEM of at least 3 independent experiments. P≤0.05, *P≤0.01.
S2271	Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Pharmacol, 2021, 12:632201 Molecules, 2021, 26(5)1210 Biology (Basel), 2021, 10(3)250
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.	J Virol, 2021, JVI.01297-20 Life Sci Alliance, 2020, 28;3(6) pii: e202000735 EMBO J, 2019, 15;38(10):e101638
S9634	Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.	Anticancer Res, 2018, 38(10):5709-5716
S7025	Embelin Embelin (Embelic Acid, NSC 91874), 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.	Cancers (Basel), 2021, 13(14)3585 Cell Host Microbe, 2018, 24(5):689-702 Am J Pathol, 2018, 188(2):404-416	(d) Representative plots of apoptosis in Jurkat cells treated with vehicle only, BIO, CN585, Embelin (Emb), BIO plus CN585 or BIO plus CN585 plus Emb.
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).	Theranostics, 2021, 11(18):9009-9021 Cell Rep, 2021, 35(6):109112 Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X	Parental or rVCR RD cells were either left untreated (UT) or exposed to 40 μM of LCL161 in the absence or presence of PSC-833 (10 μM) for 48 h before analysis of DNA fragmentation using PI staining and flow cytometry (data shown are mean + SD, n = 3). , p < 0.05, , p < 0.01, **, p < 0.001.

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 (TL32711) Birinapant (TL32711) is a SMAC mimetic antagonist, mostly to cIAP1 with K_d 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.	Sci Adv, 2021, 7(28)eabf4408 Nat Commun, 2021, 12(1):2482 EMBO Mol Med, 2021, e13466	Western blot analysis of XIAP and cIAP1 expression and PARP cleavage in H460, A549 and 34LU cells pre-treated with vorinostat or entinostat for 6h followed by the SMAC mimetic birinapant for 24h.
S7010	GDC-0152 GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with K_i 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.	Apoptosis, 2020, 21 Cell Death Dis, 2020, 11(8):680 Theranostics, 2019, 9(9):2424-2438	Inhibitor of Apoptosis Proteins (IAPs) were involved in MCP-1/IL-6 production under high dose TNF-α stimulation. A. hUC-MSCs (2x104 in 96-well plates) were pretreated for 2h with the IAP inhibitor GDC-0152 at increasing concentrations (0-1000 nM), then stimulated with TNF-α (20 ng/ml, 1.2 nM). After a further 24h, trypan blue was used to exclude cell toxicity. SN was collected and IL-6 and MCP-1 concentrations were measured by ELISA. B. hUC-MSCs(5×105 in T25 bottle) were pretreated with GDC-0152(1000nM) for 2 h, then stimulated with TNF-α (20 ng/ml, 1.2 nM). 24 hours later, protein from nucleus and cytoplasma were extracted separately and the amount of NF-kB were detected by Western blot. Data are as mean±SEM of triplicate measurements; p<0.05, p<0.01, **p<0.001 when compared to untreated cells. These experiments were repeated 3 times with the same results, using clone 69 and another TNF-α sensitive clone (clone 120003).
S2754	Xevinapant (AT406) Xevinapant (AT406, ARRY-334543, Debio1143, 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 K_i of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1.	Theranostics, 2021, 11(18):9009-9021 Cancers (Basel), 2021, 13(14)3585 Neoplasia, 2021, 23(5):539-550	G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting.
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.	Clin Epigenetics, 2021, 13(1):37 Cell Death Dis, 2021, 12(2):140 Cell Death Dis, 2018, 9(7):732
S8681	Tolinapant (ASTX660) Tolinapant (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.