xiap

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, exhibiting antinociceptive, anti-inflammatory, and antioxidant activities in different research models.

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.

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。

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 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.

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.

Phenoxodiol (Idronoxil) activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis(XIAP), disrupts FLICE inhibitory protein(FLIP) expression, and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner. Phenoxodiol also inhibits DNA topoisomerase II.

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].

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.

BV6 is an antagonist of c-IAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.

Embelin (Embelic acid), isolated from the Japanese Ardisia herb, is an inhibitor of the X-linked inhibitor of apoptosis (IC50: 4.1 uM).

Tolinapant (ASTX660) is an orally bioavailable cIAP1/2 and XIAP antagonist that induces expression of immunogenic cell death (ICD) markers in sensitive HNSCC cell lines in vitro.

XIAP-CASP7 PPI-IN-1 is a reversible inhibitor of the XIAP:CASP7 interaction, effectively disrupting the connection between XIAP and CASP7. It selectively induces apoptosis in MCF-7 and caspase-3 low-expression (CASP3/DR) triple-negative breast cancer cells. The compound overcomes chemoresistance by down-regulating β-catenin and associated ABC transporters in paclitaxel-resistant MCF-7 cells. XIAP-CASP7 PPI-IN-1 is useful for breast cancer research.

XIAPligand 5 is an XIAP antagonist and serves as an E3 ligase ligand (E3 ligase Ligand). This compound is utilized in the synthesis of PROTACGNE-1567.

XIAP degrader-1 is a small primary amine molecule that promotes the degradation of X-linked apoptosis inhibitory protein (XIAP).

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.

MDM2/XIAP-IN-2 is a dual inhibitor targeting murine double minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP), promoting MDM2 degradation and impeding XIAP mRNA translation, thereby inhibiting cancer cell proliferation. It exhibits potent activity against the acute lymphoblastic leukemia cell line EU-1, with an IC50 of 0.3 μM [1].

MDM2/XIAP-IN-3 (compound 3e), a dual inhibitor of MDM2 and XIAP, reduces MDM2 and XIAP protein levels while increasing p53 expression, ultimately inhibiting cancer cell proliferation and inducing apoptosis [1].

MDM2/XIAP-IN-1 (compound 14) is an orally active dual inhibitor of MDM2 and XIAP, displaying anti-cancer activity with an IC50 of 0.3 μM and potential applications in cancer research [1].

XIAP BIR2/BIR2-3 inhibitor-1 (compound 3) serves as a potent dual inhibitor targeting BIR2 and BIR2-3 domains, with IC50 values of 1.9 nM and 0.8 nM, respectively. This compound is utilized in cancer research studies [1].

XIAP BIR2/BIR2-3 Inhibitor-2 is a dual inhibitor of BIR2 and BIR2-3 with IC50 values less than 1 nM. It can be used in the study of cancers [1].

XIAP BIR2/BIR2-3 Inhibitor-3 functions as a dual inhibitor targeting both BIR2 and BIR2-3 domains, exhibiting potent activity with IC50 values below 1 nM. This compound is utilized in cancer research [1].

XIAP Tracer mF-Smac, a fluorescently labeled peptide, functions as an acceptor dye in conjunction with a terbium-labeled BIR domain antibody for TR-FRET assays. The binding affinities (Kd values) are measured at 4.7 nM for BIR3 (XIAP) and 17.9 nM in XIAP polarization assays.

XIAPligand-Linker Conjugate 1 is an E3 ubiquitin ligase ligand-linker conjugate that comprises the XIAPBIR2 ligand XB2M54 and a linker. XIAPligand-Linker Conjugate 1 is applicable in the synthesis of PROTAC ERα Degrader-1.