SNIPERs-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/sniper.html SNIPERsIAP-dependent Protein Eraser, Specific and Nongenetic inhibitor of apoptosis protein IAP-dependentProtein ErasersSpecific and Non-genetic inhibitor of apoptosis protein IAP-dependent Protein Erasers (SNIPER), a class of small-moleculedegrader

2、s, is designed to induce IAP-mediated ubiquitylation and proteasomal degradation of target proteins.SNIPERs recruit IAP family of RING-type E3 ligases-cIAP1, cIAP2, and XIAP. The SNIPER chemical structure consists of selective IAPantagonist (i.e., Bestatin, MV1, and LCL161), PEG linker and peptide-

3、or small-molecule-based protein of interest (POI)-specificcomponent. Unlike the chimeric molecules that recruit von Hippel-Lindau and cereblon ubiquitin ligases, SNIPERs inducesimultaneous degradation of IAPs such as cIAP1 and XIAP along with the target proteins.www.MedChemE 1 HYPERLINK https:/www.M

4、edChemE/Targets/sniper.html SNIPERs HYPERLINK https:/www.MedChemE/Targets/sniper.html HYPERLINK https:/www.MedChemE/Targets/sniper.html Inhibitors HYPERLINK https:/www.MedChemE/biotin-bs.html Biotin-BS HYPERLINK https:/www.MedChemE/biotin-bs.html HYPERLINK https:/www.MedChemE/bznh-bs.html BzNH-BSCat

5、. No.: HY-111879 Cat. No.: HY-111878Biotin-BS contains two different ligands,methyl-bestatin (MeBS) for cIAP1 and biotin, whichare connected by linkers. MeBS as a ligand forcellular inhibitor of apoptosis protein 1 (cIAP1)ubiquitin ligase.BzNH-BS contains two different ligands,methyl-bestatin (MeBS)

6、 for cIAP1 andbenzoyl-amide, which are connected by linkers.MeBS as a ligand for cellular inhibitor ofapoptosis protein 1 (cIAP1) ubiquitin ligase.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.M

7、edChemE/protac-ar-degrader-4.html PROTAC HYPERLINK https:/www.MedChemE/protac-ar-degrader-4.html HYPERLINK https:/www.MedChemE/protac-ar-degrader-4.html AR HYPERLINK https:/www.MedChemE/protac-ar-degrader-4.html HYPERLINK https:/www.MedChemE/protac-ar-degrader-4.html Degrader-4 HYPERLINK https:/www.

8、MedChemE/protac-ar-degrader-4.html HYPERLINK https:/www.MedChemE/protac-ar-degrader-4-tfa.html PROTAC HYPERLINK https:/www.MedChemE/protac-ar-degrader-4-tfa.html HYPERLINK https:/www.MedChemE/protac-ar-degrader-4-tfa.html AR HYPERLINK https:/www.MedChemE/protac-ar-degrader-4-tfa.html HYPERLINK https

9、:/www.MedChemE/protac-ar-degrader-4-tfa.html Degrader-4 HYPERLINK https:/www.MedChemE/protac-ar-degrader-4-tfa.html HYPERLINK https:/www.MedChemE/protac-ar-degrader-4-tfa.html TFACat. No.: HY-111848 Cat. No.: HY-111848APROTAC AR Degrader-4 comprises a IAP ligand bindinggroup, a linker and an Androge

10、n Receptor (AR)binding group. PROTAC AR Degrader-4 is an ARdegrader. Degradation inducers based on cIAP1 arecalled specific and non-genetic IAP-dependentprotein erasers (SNIPERs).PROTAC AR Degrader-4 comprises a IAP ligand bindinggroup, a linker and an Androgen Receptor (AR)binding group. PROTAC AR

11、Degrader-4 is an ARdegrader. Degradation inducers based on cIAP1 arecalled specific and non-genetic IAP-dependentprotein erasers (SNIPERs).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/prot

12、ac-crabp-ii-degrader-1.html PROTAC HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-1.html HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-1.html CRABP-II HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-1.html HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-1.html Degrader

13、-1 HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-1.html HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-2.html PROTAC HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-2.html HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-2.html CRABP-II HYPERLINK https:/www.MedChemE/pro

14、tac-crabp-ii-degrader-2.html HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-2.html Degrader-2Cat. No.: HY-111840 Cat. No.: HY-111841PROTAC CRABP-II Degrader-1 is a potent cellularretinoic acid binding protein (CRABP-II) degraderbased on IAP ligand.PROTAC CRABP-II Degrader-2 is a potent cellu

15、larretinoic acid binding protein (CRABP-II) degraderbased on IAP ligand.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-3.html PROTAC HYPERLINK https:/www.MedChem

16、E/protac-crabp-ii-degrader-3.html HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-3.html CRABP-II HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-3.html HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-3.html Degrader-3 HYPERLINK https:/www.MedChemE/protac-crabp-ii-degrader-3.htm

17、l HYPERLINK https:/www.MedChemE/protac-er-alpha-degrader-2.html PROTAC HYPERLINK https:/www.MedChemE/protac-er-alpha-degrader-2.html HYPERLINK https:/www.MedChemE/protac-er-alpha-degrader-2.html ER HYPERLINK https:/www.MedChemE/protac-er-alpha-degrader-2.html HYPERLINK https:/www.MedChemE/protac-er-

18、alpha-degrader-2.html Degrader-2Cat. No.: HY-111842 Cat. No.: HY-111846PROTAC CRABP-II Degrader-3 is a potent cellularretinoic acid binding protein (CRABP-II) degraderbased on IAP ligand.PROTAC ER Degrader-2 comprises a IAP ligandbinding group, a linker and an estrogen receptor (ER) binding group. P

19、ROTAC ER Degrader-2 isan ER degrader. Maximal ER degradation at 30 Mconcentration in human mammary tumor MCF7 cells.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.88%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/prota

20、c-rar-degrader-1.html PROTAC HYPERLINK https:/www.MedChemE/protac-rar-degrader-1.html HYPERLINK https:/www.MedChemE/protac-rar-degrader-1.html RAR HYPERLINK https:/www.MedChemE/protac-rar-degrader-1.html HYPERLINK https:/www.MedChemE/protac-rar-degrader-1.html Degrader-1 HYPERLINK https:/www.MedChem

21、E/protac-rar-degrader-1.html HYPERLINK https:/www.MedChemE/sniper-abl-013.html SNIPER(ABL)-013Cat. No.: HY-111844 Cat. No.: HY-111860PROTAC RAR Degrader-1 comprises a IAP ligandbinding group, a linker and a RAR ligand bindinggroup. PROTAC RAR Degrader-1 is an RAR degrader.Maximal RAR degradation at

22、30 M concentration inHT1080 cells.SNIPER(ABL)-013, conjugating GNF5 (ABL inhibitor)to Bestatin (IAP ligand) with a linker, induces thereduction of BCR-ABL protein with a DC of 2050M.Purity: 95.02%Clinical Data: No Development ReportedSize: 1 mgPurity: 98%Clinical Data: No Development ReportedSize: 1

23、 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/sniper-abl-015.html SNIPER(ABL)-015 HYPERLINK https:/www.MedChemE/sniper-abl-015.html HYPERLINK https:/www.MedChemE/sniper-abl-019.html SNIPER(ABL)-019Cat. No.: HY-111854 Cat. No.: HY-111873SNIPER(ABL)-

24、015, conjugating GNF5 (ABL inhibitor)to MV-1 (IAP ligand) with a linker, induces thereduction of BCR-ABL protein with a DC of 5 M50.SNIPER(ABL)-019, conjugating Dasatinib (ABLinhibitor) to MV-1 (IAP ligand) with a linker,induces the reduction of BCR-ABL protein with aDC of 0.3 M.50Purity: 98%Clinica

25、l Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/sniper-abl-020.html SNIPER(ABL)-020 HYPERLINK https:/www.MedChemE/sniper-abl-020.html HYPERLINK https:/www.MedChemE/sniper-abl-024.html SNIPER(ABL)-024Cat. N

26、o.: HY-111872 Cat. No.: HY-111861SNIPER(ABL)-020, conjugating Dasatinib (ABLinhibitor) to Bestatin (IAP ligand) with a linker,induces the reduction of BCR-ABL protein.SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor)to LCL161 derivative (IAP ligand) with a linker,induces the reduction of BCR-ABL pro

27、tein with aDC of 5M.50Purity: 99.44%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/sniper-abl-033.html SNIPER(ABL)-033 HYPERLINK https:/www.MedChemE/sniper-abl-033.html HYPERLINK https:/www

28、.MedChemE/sniper-abl-039.html SNIPER(ABL)-039Cat. No.: HY-111871 Cat. No.: HY-111874SNIPER(ABL)-033, conjugating HG-7-85-01 (ABLinhibitor) to LCL161 derivative (IAP ligand) with alinker, induces the reduction of BCR-ABL proteinwith a DC of 0.3 M.50SNIPER(ABL)-039, conjugating Dasatinib (ABLinhibitor

29、) to LCL161 derivative (IAP ligand) with alinker, induces the reduction of BCR-ABL proteinwith a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM,12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development

30、 ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/sniper-abl-044.html SNIPER(ABL)-044 HYPERLINK https:/www.MedChemE/sniper-abl-044.html HYPERLINK https:/www.MedChemE/sniper-abl-047.html SNIPER(ABL)-047Cat. No.: HY-111862 Cat. No.: HY-111863SNIPER(ABL)-044, conjugating HG-7-85-01 (ABLinhibitor)

31、 to Bestatin (IAP ligand) with a linker,induces the reduction of BCR-ABL protein with aDC of 10 M.50SNIPER(ABL)-047, conjugating HG-7-85-01 (ABLinhibitor) to MV-1 (IAP ligand) with a linker,induces the reduction of BCR-ABL protein with aDC of 2 M.50Purity: 98%Clinical Data: No Development ReportedSi

32、ze: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/sniper-abl-049.html SNIPER(ABL)-049 HYPERLINK https:/www.MedChemE/sniper-abl-049.html HYPERLINK https:/www.MedChemE/sniper-abl-050.html SNIPER(ABL)-050Cat. No.: HY-111851 Cat. No.: HY-111858

33、SNIPER(ABL)-049, conjugating Imatinib (ABLinhibitor) to Bestatin (IAP ligand) with a linker,induces the reduction of BCR-ABL protein with aDC of 100 M.50SNIPER(ABL)-050, conjugating Imatinib (ABLinhibitor) to MV-1 (IAP ligand) with a linker,induces the reduction of BCR-ABL protein.Purity: 98%Clinica

34、l Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/sniper-abl-058.html SNIPER(ABL)-058 HYPERLINK https:/www.MedChemE/sniper-abl-058.html HYPERLINK https:/www.MedChemE/sniper-brd-1.html SNIPER(BR

35、D)-1Cat. No.: HY-111859 Cat. No.: HY-111875SNIPER(ABL)-058, conjugating Imatinib (ABLinhibitor) to LCL161 derivative (IAP ligand) with alinker, induces the reduction of BCR-ABL proteinwith a DC of 10 M.50SNIPER(BRD)-1, consists of an IAP antagonistLCL-161 derivative and a BET inhibitor, (+)-JQ-1,con

36、nected by a linker. SNIPER(BRD)-1 induces thedegradation of BRD4 via the ubiquitin-proteasomepathway.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.40%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/sniper-er-110.html SNIPER(ER)-110 HYPERLI

37、NK https:/www.MedChemE/sniper-er-110.html HYPERLINK https:/www.MedChemE/sniper-er-87.html SNIPER(ER)-87Cat. No.: HY-122825 Cat. No.: HY-129619SNIPER(ER)-110 consists of a IAP ligand and anestrogen ligand, connected by a linker.SNIPER(ER)-51 induces estrogen receptor (ER)protein degradation with DC s of 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgSNIPER(ER)-87 consists of an inhibitor ofapoptosis protein (IAP) ligand LCL161 deriva