ciap1

XIAP cIAP1 antagonist-1 is a potent, orally active XIAP cIAP1 antagonist with an EC50 of 5.1 nM for XIAP and 0.32 nM for cIAP1, and dose-dependently inhibits tumor growth in vivo.

cIAP1 Ligand-Linker Conjugates 1 is composed of an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 1, is particularly useful in the development of SNIPERs[1].

cIAP1 ligand 1 (E3 ligase Ligand 12) is an apoptotic protein ligand based on the LCL161 derivative that recruits IAP ubiquitin ligases to degrade target proteins, and can be used in conjunction with androgen receptor ligands for the development of protein degradation agents that can be used in the study of prostate cancer.

cIAP1 Ligand-Linker Conjugates 7 is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a PROTAC linker. It is utilized in the design of SNIPERs[1].

cIAP1 ligand 2, a derivative of LCL161, is an IAP ligand that can be connected to the ABL ligand for protein via a linker, resulting in the formation of SNIPER.

cIAP1 Ligand-Linker Conjugates 16 refers to a specific type of ligase ligand-linker conjugate, possessing the ability to engage with E3 ligases, which finds application in the synthesis of PROTACs.

cIAP1 Ligand-Linker Conjugates 3 are chemical compounds comprising an IAP ligand designed specifically for the E3 ubiquitin ligase and a PROTAC linker. These conjugates, denoted as cIAP1 Ligand-Linker Conjugates 3, find utility in the design of SNIPERs, short for Specific and Non-genetic IAP-dependent Protein Erasers [1].

cIAP1 Ligand-Linker Conjugates 11 Hydrochloride is a chemical compound comprising an IAP ligand that targets the E3 ubiquitin ligase and a PROTAC linker, mainly used in the development of SNIPERs for targeted protein degradation[1].

cIAP1 Ligand-Linker Conjugates 15 hydrochloride is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker, useful in the development of SNIPERs [1].

cIAP1 Ligand-Linker Conjugates 9 feature an IAP ligand specifically targeting the E3 ubiquitin ligase, along with a PROTAC linker. It is valuable tools for developing SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 6 hydrochloride combines an IAP ligand for the E3 ubiquitin ligase with a PROTAC linker, and is utilized for designing SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 14 consist of an IAP ligand that targets the E3 ubiquitin ligase and a PROTAC linker. These conjugates, known as cIAP1 Ligand-Linker Conjugates 14, are used in the development of SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 2 is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a PROTAC linker. This compound is particularly useful in the design of SNIPERs [1].

cIAP1 Ligand-Linker Conjugates 11 is a chemical compound that combines an IAP ligand specifically designed for the E3 ubiquitin ligase with a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 11, is useful in the development of SNIPERs[1], allowing for the targeted degradation of proteins.

cIAP1 Ligand-Linker Conjugates 4 is a chemical compound that comprises an IAP ligand specifically designed for the E3 ubiquitin ligase and a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 4, has the potential to be utilized in the development of SNIPERs[1].

cIAP1-IN-D19 is an inhibitor of E3 ligase activity of cIAP1.

cIAP1 Ligand-Linker Conjugates 8 comprises an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound is specifically utilized for the purpose of SNIPER design[1].

cIAP1 Ligand-Linker Conjugates 12 is a chemical compound that combines an IAP ligand, which targets the E3 ubiquitin ligase, with a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 12, is valuable for creating SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 2 Hydrochloride is a chemical compound that combines an IAP ligand, targeting the E3 ubiquitin ligase, with a PROTAC linker and is utilized in the creation of SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 13, containing an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker, are utilized in the development of SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 10 comprise of an IAP ligand and a PROTAC linker, which facilitates the design of SNIPERs. These conjugates incorporate an IAP ligand that interacts with the E3 ubiquitin ligase, and a PROTAC linker. SNIPERs can be developed using cIAP1 Ligand-Linker Conjugates 10.

cIAP1 Ligand-Linker Conjugates 15 consists of an IAP ligand that targets the E3 ubiquitin ligase, along with a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 15, is suitable for the development of SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 5 is a chemical compound consisting of an IAP ligand that targets the E3 ubiquitin ligase, and a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 5, is specifically designed for the development of SNIPERs[1].

AZD5582 TFA is a potent IAP antagonist that binds to the BIR3 domain of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM, respectively.AZD5582 TFA induces apoptosis.

HM90822 is a novel synthetic apoptotic protein (IAP) antagonist that induces apoptosis in human pancreatic cancer cells through proteasome-dependent degradation of IAPs containing the BIR2 3 structural domain.HM90822 inhibits the expression of XIAP and cIAP1 2 proteins in HM822-sensitive Panc-1 and BxPC-3 cells, induces ubiquitylation of IAPs and promotes induces IAP ubiquitination and promotes proteasome-dependent IAP degradation.

Birinapant (TL32711) is a synthetic small molecule that is both a peptidomimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.

SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains (IC50: 1.39 nM). It acts as an extremely potent antagonist of XIAP.

AZD5582 acetate is an inhibitor of IAPs, which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.

LCL161, a SMAC mimetic, effectivity binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP).

ICCB-19 hydrochloride (ICCB-19 HCl) is an inhibitor of TRADD (TNFRSF1A Associated Via Death Domain). It binds to a pocket on the N-terminal TRAF2-binding domain of TRADD (TRADD-N), which interacts with the C-terminal domain (TRADD-C) and TRAF2 to modulate the ubiquitination of RIPK1 and beclin 1.

ZLDI-8 is an inhibitor of Notch activating/cleaving enzyme ADAM-17 and inhibits the cleavage of Notch protein.

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.

GDC-0152 is a potent inhibitor of IAPs.

AZD5582 is an inhibitor of IAPs, which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. It induces apoptosis.

Xevinapant (Debio-1143) 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.

Ch55-O-C3-NH2, also known as RAR ligand 1, is a ligand derived from the Ch55 compound that specifically targets RAR. Through a linker, Ch55-O-C3-NH2 interacts with cIAP1 ligand Bestatin to form SNIPER[1].

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].

Estrone-N-O-C1-amido (ERα ligand 1) is an estrogen ligand derivative of Estrone that specifically binds to estrogen receptor α (ERα). With a linker, it complexes with the cIAP1 ligand Bestatin, forming SNIPER[1].

ZLM-66 is a doravirine analogue and a potent inhibitor of non-nucleoside reverse transcriptases (NNRTIs), acting on wild-type HIV-1 reverse transcriptase (IC50: 41 nM), wild-type HIV-1 (EC50: 13 nM) and cIAP1 (EC50: 0.32 nM). ZLM-66 can be used in AIDS research.

PROTAC AR Degrader-4, an Androgen Receptor (AR) degrader, incorporates an IAP ligand binding group, a linker, and an AR binding group. It represents a class of degradation inducers known as specific and non-genetic IAP-dependent protein erasers (SNIPERs) [1], operating through a mechanism involving cIAP1.

TD1092, a pan-IAP degrader, effectively degrades cIAP1, cIAP2, and XIAP, catalyzing the activation of Caspase 3/7 and fostering apoptosis in cancer cells through IAP degradation. It also obstructs the TNFα-mediated NF-κB pathway, diminishing the phosphorylation of IKK, IkBα, p65, and p38, and operates as a PROTAC. This compound is utilized in cancer research [1].

MX106 is a survivin inhibitor which induces degradation of XIAP and/or cIAP1, and suppresses genotoxic NF-kappaB activation.

PROTAC RAR Degrader-1, an RAR degrader, consists of a cIAP1 ligand binding group, a linker, and an RAR ligand binding group. It achieves maximal RAR degradation at a concentration of 30 μM in HT1080 cells. Degradation inducers that utilize cIAP1 are known as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

ATRA-hydroxyimino, also known as CRABP-II ligand 1, is a chemical compound derived from Retinoic acid (ATRA). This compound binds to the cIAP1 ligand, specifically Bestatin, through a linker, resulting in the formation of a complex called SNIPER. The purpose of this complex is to degrade CRABP-II within IMR-32 cells[1].

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

BzNH-BS is a chemical compound comprising two distinct ligands: methyl-bestatin (MeBS) for cIAP1 and benzoyl-amide. The ligands are interconnected through linkers. MeBS functions as a ligand for cIAP1, a ubiquitin ligase involved in cellular inhibition of apoptosis processes [1].

MX107 is a survivin inhibitor which induces degradation of XIAP and/or cIAP1, and suppresses genotoxic NF-kappaB activation.

Xevinapant hydrochloride (AT-406 HCl) , an orally active antagonist of multiple inhibitor of apoptosis proteins(IAP), inhibits progression of human ovarian Y 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.

PROTAC CRABP-II Degrader-3 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on [cIAp1].

API-1 (NSC-177223) is a potent inhibitor of Akt. It induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis .