IAP (Inhibitors of Apoptosis) is a family of functionally and structurally related proteins, which serve as endogenous inhibitors of programmed cell death (apoptosis). A common feature of all IAPs is the presence of a BIR in one to three copies. The human IAP family consists of 8 members, and IAP homologs have been identified in numerous organisms. The members of the IAPs included IAPs, Cp-IAP, Op-IAP, XIAP, c-IAPl, C-IAP2, NAIP, Livin and Survivin. The best characterized IAP is XIAP, which binds caspase-9, caspase-3 and caspase 7, thereby inhibiting their activation and preventing apoptosis. Also cIAP1 and cIAP2 have been shown to bind caspases, although how the IAPs inhibit apoptosis mechanistically at the molecular level is not completely understood.


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XIAP BIR2/BIR2-3 inhibitor-1

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[1].

  • CAS Number: 1609384-59-9
  • MF: C72H96N16O14
  • MW: 1409.63
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Embelin

Embelin is a cell-permeable benzoquinone compound that exhibits antitumor properties. Specifically antagonizes XIAP-mediated inhibition of caspase-9 activation by directly targeting the Smac and caspase-9 binding domain BIR3 (IC50 = 4.1 uM in a competitive binding assay with Smac peptide).IC50 value: 4.1 uM [1]Target: XIAPin vitro: Embelin induced activation of caspase-9 and embelin-induced apoptosis was prevented by caspase inhibitors [2]. Treatment with subtoxic doses of Embelin broadly sensitized malignant glioma cells to TRAIL-mediated apoptosis. Notably, human astrocytes were not significantly affected by the combined treatment consisting of Embelin and TRAIL. Combined treatment with Embelin and TRAIL augmented the activation of initiator caspases-8/-9 and effector caspases-3/-7, respectively [3]. in vivo: Embelin inhibited topical edema in the mouse ear, leading to substantial reductions in skin thickness and tissue weight, inflammatory cytokine production, neutrophil-mediated myeloperoxidase activity, and various histopathological indicators. Furthermore, embelin was effective at reducing inflammatory damage induced by chronic TPA exposure [4]. Embelin (10, 30 or 50mg/kg body weight) was administrated daily per oral route for 7days. Embelin significantly attenuated DSS-induced DAI scores and tissue MPO accumulation, which implied that it suppressed weight loss, diarrhea, gross bleeding, and the infiltrations of immune cells. Embelin administration also effectively and dose-dependently prevented shortening of colon length and enlargement of spleen size [5].

  • CAS Number: 550-24-3
  • MF: C17H26O4
  • MW: 294.386
  • Catalog: IAP
  • Density: 1.131
  • Boiling Point: 431.9±45.0 °C at 760 mmHg
  • Melting Point: 145-146 ºC
  • Flash Point: 229.1±25.2 °C

XIAP BIR2/BIR2-3 inhibitor-3

XIAP BIR2/BIR2-3 inhibitor-3 is a dual inhibitor of BIR2 and BIR2-3 with IC50s less than 1 nM. XIAP BIR2/BIR2-3 inhibitor-3 can used in study cancers[1].

  • CAS Number: 1434125-52-6
  • MF: C86H106N18O16S2
  • MW: 1712.00
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BV-6

BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.

  • CAS Number: 1001600-56-1
  • MF: C70H96N10O8
  • MW: 1205.57000
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AZD 5582 dihydrochloride

AZD5582 dihydrochloride is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis[1].

  • CAS Number: 1883545-51-4
  • MF: C58H80Cl2N8O8
  • MW: 1088.21
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MV1

MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand[1].

  • CAS Number: 1001600-54-9
  • MF: C33H44N4O5
  • MW: 576.73
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SM-164

SM-164 is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.

  • CAS Number: 957135-43-2
  • MF: C62H84N14O6
  • MW: 1121.42000
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MX69

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

  • CAS Number: 1005264-47-0
  • MF: C27H26N2O4S
  • MW: 474.5794
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AT406 (SM-406)

AT-406 is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM, respectively.

  • CAS Number: 1071992-99-8
  • MF: C32H43N5O4
  • MW: 561.715
  • Catalog: IAP
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 840.5±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 462.1±34.3 °C

MDM2/XIAP-IN-3

MDM2/XIAP-IN-3 (compound 3e) is a dual MDM2/XIAP inhibitor. MDM2/XIAP-IN-3 reduces MDM2 and XIAP protein levels and increases p53 expression, thereby inhibiting cancer cell growth and causing cell death[1].

  • CAS Number: 2925583-17-9
  • MF: C29H30N2O5S
  • MW: 518.62
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Birinapant

Birinapant, a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively.

  • CAS Number: 1260251-31-7
  • MF: C42H56F2N8O6
  • MW: 806.94
  • Catalog: IAP
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 1090.5±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 613.3±34.3 °C

Xevinapant hydrochloride

Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors[1][2].

  • CAS Number: 1071992-57-8
  • MF: C32H44ClN5O4
  • MW: 598.18
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AZD5582

AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively). IC50 value: 15/21/15 nM (cIAP1/cIAP2/XIAP) [1]Target: IAPs inhibitorAZD5582 causes cIAP1 degradation and induces apoptosis in the MDA-MB-231 breast cancer cell line at subnanomolar concentrations in vitro. When administered intravenously to MDA-MB-231 xenograft-bearing mice, AZD5582 results in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg. Antiproliferative effects are observed with AZD5582 in only a small subset of the over 200 cancer cell lines examined, consistent with other published IAP inhibitors [1]. AZD5582 significantly enhanced apoptosis induced by the death receptor (DR) agonist tumour necrosis factor-related apoptosis-inducing ligand (TRAIL). Importantly, killing by TRAIL plus AZD5582 was independent of adverse prognostic features including TP53 deletion which is strongly associated with chemoresistance in CLL [2].

  • CAS Number: 1258392-53-8
  • MF: C58H78N8O8
  • MW: 1015.289
  • Catalog: IAP
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 1207.3±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 683.9±34.3 °C

ASTX660

ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).

  • CAS Number: 1799328-86-1
  • MF: C30H42FN5O3
  • MW: 539.68
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SM-433

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)[1].

  • CAS Number: 1071992-81-8
  • MF: C32H43N5O4
  • MW: 561.71
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Hydroxy-4-methylbenzoic acid

4-Methylsalicylic acid is a salicylic acid. 4-Methylsalicylic acid derivative is a selective tissue-nonspecific alkaline phosphatase (TNAP) and intestinal alkaline phosphatase (IAP) inhibitor[1].

  • CAS Number: 50-85-1
  • MF: C8H8O3
  • MW: 152.147
  • Catalog: IAP
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 315.2±30.0 °C at 760 mmHg
  • Melting Point: 173-177 °C(lit.)
  • Flash Point: 158.6±21.1 °C

UC 112

UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).IC50 value: 0.7-3.4 uM (Cell assay) [1]Target: IAP inhibitorin vitro: UC-112 also potently inhibits the growth of P-glycoprotein (P-gp)-overexpressed multidrug-resistant cancer cells, strongly activates caspase-3/7 and caspase-9 activities, and selectively downregulates survivin level at a concentration as low as 1 μM. Coincubation of UC-112 with a known proteasome inhibitor Z-Leu-Leu-Leu-CHO (MG-132) rescued survivin inhibition, consistent with the anticipated mechanism of action for UC-112 [1].in vivo: As a single agent, UC-112 strongly inhibits tumor growth and reduces both X chromosome-linked IAP and survivin levels in an A375 human melanoma xenograft model in vivo [1].

  • CAS Number: 383392-66-3
  • MF: C22H24N2O2
  • MW: 348.43800
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Polygalacin D

Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum (Jacq.) 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[1]

  • CAS Number: 66663-91-0
  • MF: C57H92O27
  • MW: 1209.324
  • Catalog: Apoptosis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LBW242

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[1].

  • CAS Number: 867324-12-7
  • MF: C27H42N4O2
  • MW: 454.64800
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Isolinderalactone

Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2 activation in endothelial cells[1]. Isolinderalactone suppresses the expression of B-cell lymphoma 2 (Bcl-2), survi

  • CAS Number: 957-66-4
  • MF: C15H16O3
  • MW: 244.29
  • Catalog: Bcl-2 Family
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AT-IAP

A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively; exhibits MDA-MB-231 cell proliferation inhibition with IC50 of 4.4 nM; decreases basal and TNF-α-induced cIAP-1 expression in CaP cells, switches TNF-α signaling from pro-survival to pro-apoptotic and increases radiation sensitivity of CaP cells in co-culture with THP-1 cells; shows in vivo efficacy in Balb/c scid mice bearing MDA-MB-231 xenografts.

  • CAS Number: 1403898-55-4
  • MF: C29H40FN5O2
  • MW: 509.659
  • Catalog: IAP
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 678.3±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 364.0±31.5 °C

CUDC-427

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

  • CAS Number: 1446182-94-0
  • MF: C29H36N6O4S
  • MW: 564.69900
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SM-1295

SM-1295 is a potent, selective cIAP1 and cIAP2 inhibitor with Ki of <10 nM, displays >900-fold for cIAP1 over XIAP; potently inhibits cell growth in the MDA-MB-231 and SK-OV-3 cancer cell lines and induces apoptosis at low nanomolar concentrations; efficiently induces degradation of cIAP1 protein in cancer cells, as well as cleavage of PARP, caspase-8, and caspase-3; induces cell death in a TNFα-dependent manner in both MDA-MB-231 and SK-OV-3 cancer cell lines.

  • CAS Number: 1562375-46-5
  • MF: C29H36BrN5O4
  • MW: 598.542
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Anticancer agent 127

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[1].

  • CAS Number: 2410953-19-2
  • MF: C26H37FN4O6S
  • MW: 552.66
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

10,11-methylenedioxycamptothecin

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[1][2].

  • CAS Number: 135415-73-5
  • MF: C21H16N2O6
  • MW: 392.36200
  • Catalog: Apoptosis
  • Density: 1.64g/cm3
  • Boiling Point: 812.1ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 445ºC

LCL161

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.

  • CAS Number: 1005342-46-0
  • MF: C26H33FN4O3S
  • MW: 500.629
  • Catalog: IAP
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 713.7±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 385.4±32.9 °C

Anticancer agent 128

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[1].

  • CAS Number: 2941243-62-3
  • MF: C26H38N4O4
  • MW: 470.60
  • Catalog: IAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GDC-0152

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

  • CAS Number: 873652-48-3
  • MF: C25H34N6O3S
  • MW: 498.641
  • Catalog: IAP
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sanggenon G

Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). Sanggenon G binds specifically to the BIR3 domain of XIAP with a binding affinity of 34.26 μM. Sanggenon G enhances caspase activation[1].

  • CAS Number: 85698-31-3
  • MF: C40H38O11
  • MW: 694.72
  • Catalog: Caspase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A