1、 HYPERLINK https:/www.MedChemE/Targets/IAP.html IAPIAP (Inhibitor of apoptosis) proteins, a family of anti-apoptotic proteins, have an important role in evasion of apoptosis, as they canboth block apoptosis-signaling pathways and promote survival. Eight members of this family have been described in

2、humans(BIRC1/NAIP, BIRC2/cIAP1, BIRC3/cIAP2, BIRC4/XIAP, BIRC5/Survivin, BIRC6/Apollon, BIRC7/ML-IAP and BIRC8/ILP2).IAP genes encode proteins that directly bind and inhibit caspases, and thus play a critical role in deciding cell fate. The IAPs are inturn regulated by endogenous proteins (second mi

3、tochondrial activator of caspases and Omi) that are released from themitochondria during apoptosis. IAP protein family members are frequently overexpressed in cancer and contribute to tumor cellsurvival, chemo-resistance, disease progression, and poor prognosis. Targeting critical apoptosis regulato

4、rs, like IAPs, is anattractive therapeutic way undertaken for the development of new classes of therapies for cancer.Although best known for their ability to regulate caspases, IAPs also influence ubiquitin (Ub)-dependent pathways that modulateinnate immune signaling via activation of NF-B. Several

5、members of the IAP family regulate innate and adaptive immunity throughmodulation of signal transduction pathways, cytokine production, and cell survival. The regulation of immunity by the IAPs isprimarily mediated through the ubiquitin ligase function of cIAP1, cIAP2, and XIAP, the targets of which

6、 impact NF-B and MAPKsignalling pathways.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/IAP.html IAP HYPERLINK https:/www.MedChemE/Targets/IAP.html HYPERLINK https:/www.MedChemE/Targets/IAP.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/IAP.html HYPERLINK https:/www.MedChemE/Targets/IAP

7、.html & HYPERLINK https:/www.MedChemE/Targets/IAP.html HYPERLINK https:/www.MedChemE/Targets/IAP.html Antagonists HYPERLINK https:/www.MedChemE/apg-1387.html APG-1387 HYPERLINK https:/www.MedChemE/apg-1387.html HYPERLINK https:/www.MedChemE/ASTX660.html ASTX660Cat. No.: HY-125593 Cat. No.: HY-109565

8、APG-1387, a bivalent SMAC mimetic and an IAPantagonist, blocks the activity of IAPs familyproteins (XIAP, cIAP-1, cIAP-2, and ML-IAP).APG-1387 induces degradation of cIAP-1 and XIAPproteins, as well as caspase-3 activation and PARPcleavage, which leads to apoptosis.ASTX660 is an orally bioavailable

9、dual antagonistof cellular inhibitor of apoptosis protein (cIAP)and X-linked inhibitor of apoptosis protein (XIAP).Purity: 99.46%Clinical Data: Phase 2Size: 1 mg, 5 mg, 10 mgPurity: 99.60%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AZD5582.

10、html AZD5582 HYPERLINK https:/www.MedChemE/AZD5582.html HYPERLINK https:/www.MedChemE/azd5582-dihydrochloride.html AZD5582 HYPERLINK https:/www.MedChemE/azd5582-dihydrochloride.html HYPERLINK https:/www.MedChemE/azd5582-dihydrochloride.html dihydrochlorideCat. No.: HY-12600 Cat. No.: HY-110346AZD558

11、2 is an antagonist of the inhibitor ofapoptosis proteins (IAPs), which binds to the BIR3domains cIAP1, cIAP2, and XIAP with IC s of 15,5021, and 15 nM, respectively. AZD5582 inducesapoptosis.AZD5582 dihydrochloride is an antagonist of theinhibitor of apoptosis proteins (IAPs), which bindsto the BIR3

12、 domains cIAP1, cIAP2, and XIAP withIC s of 15, 21, and 15 nM, respectively. AZD558250induces apoptosis.Purity: 98.11%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Birinapant.h

13、tml Birinapant(TL32711) Cat. No.: HY-16591 HYPERLINK https:/www.MedChemE/BV6.html BV6Cat. No.: HY-16701Birinapant (TL32711), a bivalent Smac mimetic, isa potent antagonist for XIAP and cIAP1 with K s ofd45 nM and less than 1 nM, respectively.BV6 is an antagonist of cIAP1 and XIAP, members ofthe inhi

14、bitors of apoptosis (IAP) family.Purity: 99.70%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.84%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/CUDC-427.html CUDC-427 HYPERLINK https:/www.MedChemE/CUDC-42

15、7.html HYPERLINK https:/www.MedChemE/embelin.html Embelin(GDC-0917) Cat. No.: HY-15835 (Embelic acid; Emberine; NSC 91874) Cat. No.: HY-17473CUDC-427 is a potent second-generationpan-selective IAP antagonist, used for treatment ofvarious cancers.Embelin (Embelic acid), a potent, nonpeptidic XIAPinhi

16、bitor (IC =4.1 M), inhibits cell growth,50induces apoptosis, and activates caspase-9 inprostate cancer cells with high levels of XIAP.Purity: 99.01%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98.75%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg HYPERLINK h

17、ttps:/www.MedChemE/GDC-0152.html GDC-0152 HYPERLINK https:/www.MedChemE/GDC-0152.html HYPERLINK https:/www.MedChemE/isolinderalactone.html IsolinderalactoneCat. No.: HY-13638 Cat. No.: HY-N3001GDC-0152 is a potent IAPs inhibitor, and binds tothe BIR3 domains of XIAP, cIAP1, cIAP2 and the BIRdomain o

18、f ML-IAP with K values of 28 nM, 17inM, 43 nM and 14 nM, respectively.Isolinderalactone suppresses human glioblastomagrowth and angiogenic activity through theinhibition of VEGFR2 activation in endothelialcells. Isolinderalactone suppresses the expressionof B-cell lymphoma 2 (Bcl-2), survi.Purity: 9

19、9.89%Clinical Data: Phase 1Size: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/lbw242.html LBW242 HYPERLINK https:/www.MedChemE/lbw242.html HYPERLINK ht

20、tps:/www.MedChemE/LCL161.html LCL161Cat. No.: HY-15519 Cat. No.: HY-15518LBW242, a 3-mer and Smac mimetic, is a potent andorally active proapoptotic IAP inhibitor. LBW242shows effects on mutant FLT3-expressing cells.LBW242 has activity against multiple myeloma, andpotentiates TRAIL- and anticancer d

21、rug-mediatedcell death of ovarian cancer cells.LCL161 is a IAP inhibitor which inhibits XIAP inHEK293 cell and cIAP1 in MDA-MB-231 cell with IC s50of 35 and 0.4 nM, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.74%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 m

22、g, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/mv1.html MV1 HYPERLINK https:/www.MedChemE/mv1.html HYPERLINK https:/www.MedChemE/MX69.html MX69Cat. No.: HY-113534 Cat. No.: HY-100892MV1 is an antagonist of IAP (inhibitor of apoptosisprotein), leads to protein knockdown ofHaloTag-fused protein

23、s when combined with HaloTagligand.MX69 is an inhibitor of MDM2/XIAP, used forcancer treatment.Purity: 99.54%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.99%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERL

24、INK https:/www.MedChemE/polygalacin-d.html Polygalacin HYPERLINK https:/www.MedChemE/polygalacin-d.html HYPERLINK https:/www.MedChemE/polygalacin-d.html DCat. No.: HY-N6064 HYPERLINK https:/www.MedChemE/sbp-0636457.html SBP-0636457(SBI-0636457; SB1-0636457) Cat. No.: HY-125378Polygalacin D (PGD) is

25、a bioactive compoundisolated from Platycodon grandiflorum (Jacq.)with anticancer and anti-proliferativeproperties.SBP-0636457 (SB1-0636457) is a SMAC mimetic, andas an IAP antagonist. SBP-0636457 binds to theBIR-domains of the IAP proteins, with a K of 0.27iM. SBP-0636457 can be used for the researc

26、h ofsolid tumors and hematologic cancers.Purity: 99.30%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.42%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/sm-1295.html SM-1295 HYPERLINK https:/www.MedChemE/sm-1295.html HYPERLINK htt

27、ps:/www.MedChemE/SM-164.html SM-164Cat. No.: HY-124181 Cat. No.: HY-15989SM-1295 is an inhibitor of apoptosis protein (IAP)antagonist, with K values of 3077 nM, 3.2 nMdand 9.5 nM for XIAP-BIR3, c-IAP1-BIR3 andc-IAP2-BIR3, respectively.SM-164 is a cell-permeable Smac mimetic compound.SM-164 binds to

28、XIAP protein containing both theBIR2 and BIR3 domains with an IC value of 1.3950nM and functions as an extremely potent antagonistof XIAP.Purity: 98.71%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.65%Clinical Data: No Development ReportedSize: 5 mg, 10 mg,

29、50 mg, 100 mg HYPERLINK https:/www.MedChemE/SM-164_Hydrochloride.html SM-164 HYPERLINK https:/www.MedChemE/SM-164_Hydrochloride.html HYPERLINK https:/www.MedChemE/SM-164_Hydrochloride.html Hydrochloride HYPERLINK https:/www.MedChemE/SM-164_Hydrochloride.html HYPERLINK https:/www.MedChemE/sm-433.html SM-433Cat. No.: HY-15989A Cat. No.: HY-138059SM-164 Hydrochloride is a cell-permeable Smacmimetic compound. SM-164 binds to XIAP proteincontaining both the BIR2 and BIR3 domains with anIC value of 1.39 nM and functions as an50extremely potent antagonist of XIAP.SM-433, a