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Search Results for " xiap "

48

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T64161	XIAP degrader-1
	XIAP degrader-1 是一种能够促进 X-连锁凋亡抑制蛋白（XIAP）降解的伯胺小分子。
T79483	MDM2/XIAP-IN-3
	MDM2/XIAP-IN-3（化合物 3e）为MDM2/XIAP双重抑制剂，能够下调MDM2与XIAP蛋白水平，提升p53表达，进而抑制癌细胞增殖并诱导细胞凋亡。
T81830	MDM2/XIAP-IN-1
	MDM2/XIAP-IN-1（compound 14）是一种口服活性的MDM2/XIAP双靶点抑制剂，展现出抗癌活性，其IC50值为0.3 μM，适用于癌症研究。
T79012	MDM2/XIAP-IN-2
	MDM2/XIAP-IN-2为MDM2（murine double minute 2）和XIAP（x-linked inhibitor of apoptosis protein）的双重抑制剂, 能够降解MDM2并抑制XIAP mRNA的翻译，进而抑制癌细胞生长。该化合物在针对急性淋巴细胞白血病细胞系EU-1的研究中显示出优秀的抑制效果，IC50值为0.3 μM。
T64302	XIAP/cIAP1 antagonist-1
	XIAP/cIAP1 antagonist-1 是一种有效的、口服具有活力的 XIAP/cIAP1 拮抗剂，能够作用于 XIAP (EC50: 5.1 nM) 和 cIAP1 (EC50: 0.32 nM)。XIAP/cIAP1 antagonist-1 能够剂量依赖性地抑制体内肿瘤生长。
T16522	Phenoxodiol 脱氢雌马酚,Dehydroequol,Idronoxil,Haginin E	Apoptosis; IAP; Caspase; Topoisomerase; p53	Apoptosis; DNA Damage/DNA Repair; Proteases/Proteasome
	Phenoxodiol (Idronoxil) 是合成genestein 的类似物，激活线粒体caspase 系统，抑制XIAP，使癌细胞对fas 介导的凋亡敏感。它在细胞周期的G1/S 期诱导细胞周期阻滞，通过独立于p53的方式上调p21WAF1。它通过稳定可分裂复合物抑制DNA 拓扑异构酶II，从而阻止DNA 复制。
T12932L	SM-164	Apoptosis; IAP	Apoptosis
	SM-164 是细胞渗透性 Smac 类似物，与含有 BIR2 和 BIR3 结构域的 XIAP 蛋白结合，IC50值为 1.39 nM，它用作XIAP 的强效拮抗剂。
T36201L	AZD5582 TFA AZD5582 TFA（1258392-53-8 free base）	Apoptosis; IAP	Apoptosis
	AZD5582 TFA 是一种有效的 IAP 拮抗剂，可与 cIAP1，cIAP2 和 XIAP 的 BIR3 结构域结合, IC50 值分别为 15，21，15 nM。AZD5582 TFA可诱导细胞凋亡。
T2080	LCL161	IAP	Apoptosis
	LCL161 是一种 SMAC 模拟物，可有效结合并抑制多种 IAP。它抑制 HEK293 细胞中 XIAP 和 MDA-MB-231细胞中 cIAP1的 IC50分别为 35 和 0.4 nM。
T14378L	AZD5582 acetate (1258392-53-8 free base)	IAP	Apoptosis
	AZD5582 acetate (1258392-53-8 free base) 是一种 IAP 抑制剂，与 BIR3 结构域 cIAP1、cIAP2 和 XIAP 结合，IC50 分别为 15、21 和 15 nM。 AZD5582 诱导细胞凋亡。
T3653	MX69	Mdm2; E1/E2/E3 Enzyme; IAP	Apoptosis; Ubiquitination
	MX69 是用于抗癌研究的一种MDM2/XIAP 抑制剂。
TQ0029	ASTX660	IAP	Apoptosis
	ASTX660 是一种口服生物可利用的 cIAP 和 XIAP 双重拮抗剂。
T6763	Xevinapant ARRY-334543,SM-406,AT406,Debio-1143	IAP	Apoptosis
	Xevinapant (Debio-1143) 是一种有效的 Smac 模拟物和 IAP 的拮抗剂，能够抑制 XIAP，cIAP1 和 cIAP2 蛋白，Ki 值分别为 66.4，1.9 和 5.1 nM。
T6428	BV6	IAP	Apoptosis
	BV6 是 c-IAP1 和 XIAP 的拮抗剂，它们是凋亡抑制剂 (IAP) 家族的成员。
T6299	GDC-0152 GDC0152	IAP	Apoptosis
	GDC-0152 是一种 IAP 抑制剂，可以与 XIAP、cIAP1和cIAP2的 BIR3 结合域，以及ML-IAP 的 BIR 结合域结合，Ki 值分别为 28 nM、17 nM、43 nM 和 14 nM。
T6007	Birinapant TL32711,比瑞那帕	Apoptosis; IAP; HIV Protease	Apoptosis; Microbiology/Virology; Proteases/Proteasome
	Birinapant (TL32711) 是一种二价 Smac 模拟物，是 XIAP 和 cIAP1的强效拮抗剂，Kd 值分别为 45 nM 和小于 1 nM。它靶向与 TRAF2 相关的 cIAP，并消除 TNF 诱导的 NF-κB 活化。
T12932	SM-164 Hydrochloride (957135-43-2 free base) SM-164 Hydrochloride	IAP	Apoptosis
	SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains(IC50 value of 1.39 nM) and functions as an extremely potent antagonist of XIAP.
T36201	AZD5582 dihydrochloride AZD 5582 dihydrochloride
	Dimeric Smac mimetic; potent inhibitor of X-linked (XIAP) and cellular (cIAP) inhibitor of apoptosis protein (IC50 values are 15, 15 and 21 nM for XIAP, cIAP1 and cIAP2 respectively). Binds to the BIR3 domain of XIAP to prevent interaction with caspase-9. Causes degradation of cIAP1 and cIAP2 and induces apoptosis in MDA-MB-231 breast cancer cells. Causes tumor regression in MDA-MB-231 xenograft-bearing mice. Hennessy et al (2013) Discovery of a novel class of dimeric Smac mimetics as potent IAP...
T69840	MX106
	MX106 is a survivin inhibitor which induces degradation of XIAP and/or cIAP1, and suppresses genotoxic NF-kappaB activation.
T14378	AZD5582	Apoptosis; IAP	Apoptosis
	AZD5582 是一种 IAP 拮抗剂，可诱导凋亡，可与 cIAP1、cIAP2 和 XIAP 的 BIR3 结构域结合，IC50值分别为 15、21和15 nM。
T23760	AT-IAP
	AT-IAP is an effective dual antagonist of XIAP and cIAP1.
T68578	A-410099.1 free base
	A-410099.1 is a novel potent xiap antagonist
T75243	SM-164 Hydrochloride
	SM-164 Hydrochloride 是一种可渗透细胞的 Smac 类似物。SM-164 与含有 BIR2 和 BIR3 结构域的XIAP 蛋白结合，IC50值为 1.39 nM，SM-164 用作XIAP 的强效拮抗剂。
T30095	APG-1387 SM 1387,SM-1387,SM1387,APG 1387l
	APG-1387 (SM-1387) is an IAP inhibitor that promotes the rapid degradation of cIAP1/2 and XIAP and exerts an anti-tumor effect on nasopharyngeal carcinoma stem cells. Studies have shown that APG-1387 combined with NPC's CDDP and 5-FU enhance chemoresensit
T18690	SNIPER(ABL)-039	Others	Others
	SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively[1].
T36317	SM-1295
	SM-1295 serves as an antagonist to the inhibitor of apoptosis protein (IAP), demonstrating dissociation constant (Kd) values of 3077 nM for XIAP-BIR3, 3.2 nM for c-IAP1-BIR3, and 9.5 nM for c-IAP2-BIR3, respectively[1][2].
T26246	T-3256336 T3256336
	T-3256336 is an orally available IAP antagonist agent that acts by selectively binding to and antagonizing protein interactions involving cellular IAP-1 (cIAP-1), cIAP-2, and X-linked IAP (XIAP).
T79247	Anticancer agent 127	IAP	Apoptosis
	Anticanceragent 127 (142D6) 是一种共价靶向 XIAP、cIAP1 以及 cIAP2 的 BIR3 结构域的IAP抑制剂，其对 XIAP、cIAP1 和 cIAP2 的 BIR3 结构域的 IC50 值分别为 12 nM、14 nM 和 9 nM，显示出抗癌活性。
T26242	SW IV-52 SW-IV-52,SW IV52,SW IV 52,SWIV52
	SW IV-52 is an XIAP-inhibitor that acts as a second mitochondria-derived activator of caspases (SMAC) mimetic.
T69845	MX107
	MX107 is a survivin inhibitor which induces degradation of XIAP and/or cIAP1, and suppresses genotoxic NF-kappaB activation.
T16905	SNIPER(BRD)-1	Others	Others
	SNIPER(BRD)-1 is a chemical compound composed of a derivative of the IAP antagonist LCL-161 and the BET inhibitor (+)-JQ-1, linked together. It promotes the degradation of BRD4 through the ubiquitin-proteasome pathway and effectively degrades cIAP1, cIAP2, and XIAP with IC50 values of 6.8 nM, 17 nM, and 49nM, respectively[1].
T78947	CST626	PROTACs	PROTAC
	CST626 (Compound 9) 为一种pan-IAP PROTAC降解剂，其在MM.1S细胞中对XIAP、cIAP1以及cIAP2的DC50分别为0.7 nM、2.4 nM和6.2 nM。
T36890	A 410099.1
	High affinity XIAP antagonist (Kd = 16 nM for the BIR3 domain of XIAP). Exhibits cytotoxicity in a wide range of cancer cell lines in vitro (EC50 = 13 nM in MDA-MB-231 cells). Also displays antitumor activity in a mouse breast cancer xenograft model. Enhances TRAIL-induced apoptosis in chronic lymphocytic leukemia (CLL) cells. Oost et al (2004) Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J.Med.Chem. 47 4417 PMID:15317454 \|Loeder et al (2009) A n...
T79248	Anticancer agent 128	IAP	Apoptosis
	Anticanceragent 128 (compound 1)作为IAP抑制剂，其通过共价作用针对XIAP、cIAP1和cIAP2的BIR3结构域。本化合物对XIAP、cIAP1和cIAP2的BIR3结构域的IC50值分别为24.9 nM、19.3 nM和10.3 nM。
T3299	Xevinapant hydrochloride AT-406 HCl,SM-406	Apoptosis; IAP	Apoptosis
	Xevinapant hydrochloride (AT-406 HCl) 是口服生物可利用的 Smac 模拟物，也是细胞凋亡蛋白抑制剂的拮抗剂。它在无细胞功能测定中有效拮抗 XIAP BIR3 蛋白，诱导细胞 cIAP1 蛋白的快速降解，并抑制各种人类癌细胞系中的癌细胞生长。它在诱导异种移植肿瘤细胞凋亡方面非常有效。
T74847	PROTAC pan-IAP degrader-1
	PROTACpan-IAP degrader-1 (Compound 9) 是一种 pan-IAPPROTAC 降解剂。PROTACpan-IAP degrader-1 在 MM.1S 细胞中降解 XIAP、cIAP1 和 cIAP2 的 DC50分别为 0.7、2.4 和 6.2 nM。
T64217	SM-433 hydrochloride
	SM-433 hydrochlorid 是一种 Smac 模拟物，是一种凋亡抑制蛋白(IAPs)抑制剂。SM-433 hydrochlorid 能够强力结合 XIAP BIR3 蛋白 (IC50<1 μM)。
T63969	SM-433
	SM-433 是 Smac 模拟物，是凋亡抑制蛋白(IAPs)的抑制剂。SM-433 对 XIAP BIR3 蛋白具有较强的亲和力 (IC50<1 μM)。
T18697	SNIPER(ER)-87	Others	Others
	SNIPER(ER)-87 is a chemical compound composed of a derivative of the inhibitor of apoptosis protein (IAP) ligand LCL161 conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen using a PEG linker. It effectively degrades the ERα protein with an IC50 value of 0.097 μM. Within cells, SNIPER(ER)-87 selectively recruits XIAP to ERα, and XIAP functions as the primary E3 ubiquitin ligase responsible for the degradation of ERα induced by SNIPER(ER)-87[1][2].
T70096	AEG40730 HCl
	AEG40730 is a potent and selective IAP antagonist and a BIR-binding tetrapeptide. AEG40730 binds to cIAP1 and cIAP2, facilitates their autoubiquitination and proteosomal degradation, and causes a dramatic reduction in RIP1 ubiquitination. Treatment with nanomolar concentrations of AEG40730 resulted in the loss of both XIAP and c-IAP1 proteins, albeit with different kinetics.
T68869	TP-110
	TP-110 is a new proteasome inhibitor, which shows potent growth inhibition in various tumor cell lines. Treatment with TP-110 for 24 h in vitro induced apoptosis in multiple myeloma cell line RPMI8226. TP-110 reduced the intrinsic inhibitor of apoptosis proteins (IAPs), cIAP-1 and XIAP, that suppress executioner caspases.
T40419	IRES-C11 IRES-C11	c-Myc	Cell Cycle/Checkpoint
	IRES-C11 is a specific inhibitor of translation that targets the internal ribosome entry site (IRES) of the c-MYC gene. It functions by blocking the interaction between heterogeneous nuclear ribonucleoprotein A1, a trans-acting factor required for c-MYC IRES activity, and its corresponding IRES. Notably, IRES-C11 does not inhibit the IRES activity of BAG-1, XIAP, and p53.
T70988	Ibulocydine
	Ibulocydine is a potent CDK inhibitor. Ibulocydine has high activity against Cdk7/cyclin H/Mat1 and Cdk9/cyclin T. Ibulocydine inhibited the growth of HCC cells more effectively than other Cdk inhibitors, including olomoucine and roscovitine, whereas ibulocydine as well as the other Cdk inhibitors and BMK-Y101 minimally influenced the growth of normal hepatocyte cells. Ibulocydine induced apoptosis in HCC cells, most likely by inhibiting Cdk7 and Cdk9. In vitro treatment of HCC cells with ibuloc...
T75010	TD1092
	TD1092 是一种泛凋亡抑制蛋白 (IAP) 降解剂，可降解 cIAP1,cIAP2和 XIAP。TD1092 激活细胞凋亡蛋白酶 (apoptosis3/7)，并通过促进 IAP 降解，导致癌细胞凋亡 (apoptosis)。同时，TD1092 还能够阻断 TNFα介导的 NF-κB 信号通路，抑制 IKK，IkBα，p65，和 p38 的磷酸化。TD1092 可作为 PROTAC，用于癌症研究。
T68980	MRK003
	MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cel...
T62822	CT1-3
	CT1-3 是一种有效的抗癌剂。CT1-3 能够调控 JNK/Bcl-2/Bax/XIAP 通路，进而诱导线粒体介导的细胞凋亡 (apoptosis)。CT1-3 可以调控 E-cadherin/Snail 轴抑制人癌细胞 (HCCs) 的上皮间充质转化 (EMT) 电位，并抑制肿瘤发生。CT1-3 在小鼠模型中具有抗肿瘤作用，且没有表现出明显的肝、肾毒性。
T83898	S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine SFN-Cys,D,L-Sulforaphane-L-cysteine
	S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine (SFN-Cys) 是一种异硫氰酸酯衍生物及第一类和第二类组蛋白去乙酰化酶（HDAC）抑制剂和抗癌剂硫代硫酸烯醇醚的活性代谢产物。它通过巯基乙酸途径酶从硫代硫酸烯醇醚经DL-硫代硫酸烯醇醚谷胱甘肽和硫代硫酸烯醇醚半胱氨酸甘肽中间体形成。SFN-Cys (20 µM) 通过创伤愈合和腔室分析实验，分别减少了U87MG和U373 MG胶质母细胞瘤细胞的侵袭和迁移。在45 µM的浓度下，它降低了对紫杉醇耐药的A549肺癌细胞（A549/T）中的α-微管蛋白、βIII-微管蛋白、司他敏1和X连锁抑制剂的凋亡（XIAP）的水平，并减少了细胞密度。使用30 µM浓度的SFN-Cys诱导U87MG和U373 MG细胞凋亡和G2/M期细胞周期停滞。
T38857	SBP-0636457 SBI-0636457,SB1-0636457,SBP-0636457
	SBP-0636457 (SB1-0636457) is a SMAC mimetic and an inhibitor of inhibitor of apoptosis (IAP) proteins. It specifically binds to the BIR-domains of IAP proteins with a Ki value of 0.27 μM. SBP-0636457 holds potential for research in the fields of solid tumors and hematologic cancers.

化合物

XIAP degrader-1

Cat.No: T64161

MDM2/XIAP-IN-3

Cat.No: T79483

MDM2/XIAP-IN-1

Cat.No: T81830

MDM2/XIAP-IN-2

Cat.No: T79012

XIAP/cIAP1 antagonist-1

Cat.No: T64302

Cat.No: T16522

Synonym: 脱氢雌马酚,Dehydroequol,Idronoxil,Haginin E

Target: Apoptosis, IAP, Caspase, Topoisomerase, p53

Cat.No: T12932L

Target: Apoptosis, IAP

Cat.No: T36201L

Synonym: AZD5582 TFA（1258392-53-8 free base）

Target: Apoptosis, IAP

Cat.No: T2080

Target: IAP

AZD5582 acetate (1258392-53-8 free base)

Cat.No: T14378L

Target: IAP

Cat.No: T3653

Target: Mdm2, E1/E2/E3 Enzyme, IAP

Cat.No: TQ0029

Target: IAP

Cat.No: T6763

Synonym: ARRY-334543,SM-406,AT406,Debio-1143

Target: IAP

Cat.No: T6428

Target: IAP

Cat.No: T6299

Synonym: GDC0152

Target: IAP

Cat.No: T6007

Synonym: TL32711,比瑞那帕

Target: Apoptosis, IAP, HIV Protease

SM-164 Hydrochloride (957135-43-2 free base)

Cat.No: T12932

Synonym: SM-164 Hydrochloride

Target: IAP

AZD5582 dihydrochloride

Cat.No: T36201

Synonym: AZD 5582 dihydrochloride

Cat.No: T69840

Cat.No: T14378

Target: Apoptosis, IAP

Cat.No: T23760

A-410099.1 free base

Cat.No: T68578

SM-164 Hydrochloride

Cat.No: T75243

Cat.No: T30095

Synonym: SM 1387,SM-1387,SM1387,APG 1387l

SNIPER(ABL)-039

Cat.No: T18690

Target: Others

Cat.No: T36317

Cat.No: T26246

Synonym: T3256336

Anticancer agent 127

Cat.No: T79247

Target: IAP

Cat.No: T26242

Synonym: SW-IV-52,SW IV52,SW IV 52,SWIV52

Cat.No: T69845

Cat.No: T16905

Target: Others

Cat.No: T78947

Target: PROTACs

Cat.No: T36890

Anticancer agent 128

Cat.No: T79248

Target: IAP

Xevinapant hydrochloride

Cat.No: T3299

Synonym: AT-406 HCl,SM-406

Target: Apoptosis, IAP

PROTAC pan-IAP degrader-1

Cat.No: T74847

SM-433 hydrochloride

Cat.No: T64217

Cat.No: T63969

Cat.No: T18697

Target: Others

Cat.No: T70096

Cat.No: T68869

Cat.No: T40419

Synonym: IRES-C11

Target: c-Myc

Cat.No: T70988

Cat.No: T75010

Cat.No: T68980

Cat.No: T62822

S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine

Cat.No: T83898

Synonym: SFN-Cys,D,L-Sulforaphane-L-cysteine

Cat.No: T38857

Synonym: SBI-0636457,SB1-0636457,SBP-0636457

Cat. No.	Product Name	Target	Signaling Pathways
T3884	Neoandrographolide Neoandrographiside,新穿心莲内酯	NOS; COX	Immunology/Inflammation; Neuroscience
	Neoandrographolide (Neoandrographiside) 是一种二萜类化合物，从穿心莲中分离得到。
T3867	Alpinetin 山姜素,(-)-alpinetin	BCL; PPAR	Apoptosis; DNA Damage/DNA Repair; Metabolism
	Alpinetin ((-)-alpinetin) 是从草豆蔻中分离得到的一种黄酮类天然产物，能够活化PPAR-γ，具有抗炎、抗菌活性。它通过抑制增殖、调节 Bcl-2 家族和 XIAP 表达、释放细胞色素 c 和激活 caspase 具有很强的抗肝癌和胰腺癌细胞作用。
T6485	Embelin NSC 91874,恩贝酸,恩贝酸/恩贝灵,Emberine,Embelic acid	Apoptosis; NF-κB; Lipoxygenase; IAP; Prostaglandin Receptor; Autophagy	Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation; Metabolism; NF-κB
	Embelin (Embelic acid) 是从日本 Ardisia 草药中分离出来的一种非肽类细胞渗透性XIAP 抑制剂，诱导口腔鳞癌细胞自噬和凋亡。它阻断 NF-kappaB 信号通路，从而抑制 NF-kappaB 调节的抗凋亡和转移基因产物。在高水平 XIAP 的前列腺癌细胞中抑制细胞生长，诱导凋亡，并激活 caspase-9。
T73876	Sanggenon G
	Sanggenon G 是一种具有细胞渗透性的有效的 X 连锁凋亡抑制蛋白 (XIAP) 抑制剂。Sanggenon G 特异性结合XIAP 的 BIR3 结构域，结合亲和力为 34.26 μM。Sanggenon G 增强caspase 激活。

天然产物

Neoandrographolide

Cat.No: T3884

Synonym: Neoandrographiside,新穿心莲内酯

Target: NOS, COX

Cat.No: T3867

Synonym: 山姜素,(-)-alpinetin

Target: BCL, PPAR

Cat.No: T6485

Synonym: NSC 91874,恩贝酸,恩贝酸/恩贝灵,Emberine,Embelic acid

Target: Apoptosis, NF-κB, Lipoxygenase, IAP, Prostaglandin Receptor, Autophagy

Cat.No: T73876

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