IAP Inhibitor

LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC₅₀s of 35 and 0.4 nM, respectively.

FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin), a Camptothecin (HY-16560) analogue, is a potent and orally active survivin inhibitor. FL118 binds to oncoprotein DDX5 (p68) to dephosphorylates and degrades DDX5. FL118 can be used for the research of cancer.

Apoptosis inducer 61 (Compound 4E) is an Apoptosis inducer. Apoptosis inducer 61 significantly downregulates the expression of BIRC3 and activates Apoptosis. Anticancer agent 313 exhibits anticancer activity against ER⁺ breast cancer cells, triple-negative breast cancer cells, and gastric cancer cells.

GDC-0152 is a potent IAPs inhibitor, and binds to the BIR3 domains of XIAP, cIAP1, cIAP2 and the BIR domain of ML-IAP with K_i values of 28 nM, 17 nM, 43 nM and 14 nM, respectively.

MX69 is an inhibitor of MDM2/XIAP, used for cancer treatment.

CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.

XIAP degrader-1, a primary amine tethered small molecule, promotes the degradation of X-linked inhibitor of apoptosis protein (XIAP).

Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.

1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC₅₀=50-58 μg/mL), with low toxicity to normal cells.

Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway. Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer.

Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum with anticancer and anti-proliferative properties. PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis

A 410099.1 is a BIRC inhibitor, with EC₅₀ values for BIRC2, BIRC3, BIRC4, BIRC7, and BIRC8 are 4.6, 9.2, 15.6, 19.9, and 93.9 nM, respectively.

UC-112 is a XIAP inhibitor with anticancer activity. UC-112 selectively downregulates and degrades survivin via the ubiquitin-mediated proteasomal degradation pathway. UC-112 reduces XIAP levels in in vivo tumor models. UC-112 activates caspase-3/7 and caspase-9, and induces cancer cell apoptosis. UC-112 is applicable to studies on melanoma, prostate cancer and cancer-related research.

SM-433, a Smac mimetic, function as inhibitor of inhibitor of apoptosis proteins (IAPs). SM-433 exhibits strong binding affinity XIAP BIR3 protein with an IC₅₀<1 μM (patent WO2008128171A2).

SM-433 hydrochlorid, a Smac mimetic, function as inhibitor of inhibitor of apoptosis proteins (IAPs). SM-433 hydrochlorid exhibits strong binding affinity XIAP BIR3 protein with an IC₅₀<1 μM (patent WO2008128171A2).

Anticancer agent 128 (compound 1) is an IAP inhibitor that covalently targets the BIR3 domains of XIAP, cIAP1, and cIAP2. Anticancer agent 128 targets the BIR3 domains of XIAP, cIAP1, and cIAP2 with IC₅₀s of 24.9 nM, 19.3 nM, and 10.3 nM, respectively.

Anticancer agent 127 (142D6) is an IAP inhibitor that covalently targets the BIR3 domains of XIAP, cIAP1, and cIAP2. Anticancer agent 127 targets the BIR3 domains of XIAP, cIAP1, and cIAP2 with IC₅₀s of 12 nM, 14 nM, and 9 nM, respectively. Anticancer agent 127 has anticancer effects.

LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer agent-mediated cell death of ovarian cancer cells.

N4Py is a bleomycin-mimetic pentadentate ligand that targets intracellular FeII and reversibly chelates a variety of transition metals. N4Py chelates induce apoptosis through two pathways: DNA cleavage via ROS generation and XIAP downregulation via ZnII chelation, with only FeII/FeIII-N4Py exhibiting potent DNA cleavage activity. The folate conjugate of N4Py targets folate receptors, can be intracellularly cleaved, and selectively kills FR-positive cancer cells. N4Py can be used in research on various cancers including nasopharyngeal epidermoid carcinoma, ovarian cancer, and mammary adenocarcinoma.

XIAP BIR2/BIR2-3 inhibitor-1 (compound 3) is a dual inhibitor of BIR2 and BIR2-3 with IC₅₀s of 1.9 and 0.8 nM, respectively. XIAP BIR2/BIR2-3 inhibitor-1 can used in study cancers.