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SNIPER

"IAPs can inhibit apoptosis by inhibiting caspase, and also exhibits the activity of E3 ubiquitin ligase. Specific and nongenetic IAP-based protein erasers (SNIPERs) are hybrid molecules that designed based on IAPs, and used to degrade the target proteins closely associated with diseases. SNIPERs (PROTACs) degrade diseases-associated proteins through human inherent ubiquitin-proteasome system. So far, many SNIPERs have been developed to treat diseases that difficult to handle by traditional methods, such as radiotherapy, chemotherapy and small molecule inhibitors, and showed promising prospects in application. PROTACs/SNIPERs are composed of three parts, including a ligand for target protein, a ligand for E3 ligase and a linker between them. All three parts are crucial for protein degradation activity of PROTACs/SNIPERs. In recent years, PROTACs (SNIPERs) have been universally used as inducers to degrade many target proteins, such as AR, ER, Era and etc."

  • SNIPER(ABL)-015
    T18685
    SNIPER(ABL)-015, conjugating GNF5 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5 μM [1].
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  • PROTAC AR Degrader-4
    T185961351169-31-7
    PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].
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    • SNIPER(ABL)-024
      T186882222355-77-1
      SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5μM[1].
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    • PROTAC ERα Degrader-2
      T186051351169-29-3
      PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].
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    • SNIPER(ABL)-039
      T186902222354-29-0
      SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively[1].
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    • SNIPER(ABL)-033
      T186892222354-18-7
      SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM[1].
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    • SNIPER(ABL)-013
      T18684
      SNIPER(ABL)-013, conjugating GNF5 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 20 μM[1].
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    • SNIPER(ABL)-047
      T18692
      SNIPER(ABL)-047, conjugating HG-7-85-01 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 2 μM[1].
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    • SNIPER(ABL)-050
      T18694
      SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker. This conjugation results in the reduction of BCR-ABL protein[1].
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    • SNIPER(ER)-110
      T18696
      SNIPER(ER)-110 comprises a cIAP1 ligand and an estrogen ligand connected by a linker. SNIPER(ER)-51 induces estrogen receptor (ER) protein degradation with DC50s of <3 nM and 7.7 nM after 4 h and 48 h, respectively [1].
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    • SNIPER(ABL)-019
      T18686
      SNIPER(ABL)-019, conjugating Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM[1].
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    • SNIPER(ABL)-058
      T186952222354-61-0
      SNIPER(ABL)-058, conjugating Imatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM[1].
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    • PROTAC CRABP-II Degrader-2
      T138371225383-38-9
      PROTAC CRABP-II Degrader-2 is a potent cIAp1-based degrader of cellular retinoic acid binding protein (CRABP-II).
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    • SNIPER(ABL)-044
      T18691
      SNIPER(ABL)-044, conjugating HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM[1].
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    • BzNH-BS
      T17706
      BzNH-BS is a chemical compound comprising two distinct ligands: methyl-bestatin (MeBS) for cIAP1 and benzoyl-amide. The ligands are interconnected through linkers. MeBS functions as a ligand for cIAP1, a ubiquitin ligase involved in cellular inhibition of apoptosis processes [1].
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    • SNIPER(TACC3)-1
      T13891
      SNIPER(TACC3)-1 targets TACC3 protein degradation via the ubiquitin-proteasome pathway.It induces cancer cell death.
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    • PROTAC RAR Degrader-1
      T186351351169-27-1
      PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].
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    • SNIPER(ABL)-049
      T18693
      SNIPER(ABL)-049, conjugating Imatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 100 μM[1].
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    • SNIPER(TACC3)-2
      T13892
      SNIPER(TACC3)-2 targets TACC3 protein degradation via the ubiquitin-proteasome pathway. It induces cancer cell death.
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    • SNIPER(ER)-87
      T186972222354-91-6
      SNIPER(ER)-87 is a chemical compound composed of a derivative of the inhibitor of apoptosis protein (IAP) ligand LCL161 conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen using a PEG linker. It effectively degrades the ERα protein with an IC50 value of 0.097 μM. Within cells, SNIPER(ER)-87 selectively recruits XIAP to ERα, and XIAP functions as the primary E3 ubiquitin ligase responsible for the degradation of ERα induced by SNIPER(ER)-87[1][2].
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    • Biotin-BS
      T17545
      Biotin-BS is a chemical compound composed of two distinct ligands: methyl-bestatin (MeBS) for cIAP1 and biotin. These ligands are interconnected through linkers. MeBS serves as a ligand specifically for the cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase[1].
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    • PROTAC CRABP-II Degrader-3
      T138381225383-41-4
      PROTAC CRABP-II Degrader-3 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on [cIAp1].
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    • SNIPER(BRD)-1
      T169052095244-54-3
      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].
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    • SNIPER(ABL)-020
      T18687
      SNIPER(ABL)-020 is a chemical compound consisting of Dasatinib, an ABL inhibitor, and Bestatin, an IAP ligand, conjugated with a linker. This compound effectively reduces the BCR-ABL protein[1].
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    • PROTAC CRABP-II Degrader-1
      T138361225383-40-3
      PROTAC CRABP-II Degrader-1 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on cIAp1.
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