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PROTAC抑制剂 Cocktails
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)-015T18685SNIPER(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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规格数量 - PROTAC AR Degrader-4T185961351169-31-7PROTAC 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].询价
- PROTAC CRABP-II Degrader-2T138371225383-38-9PROTAC CRABP-II Degrader-2 is a potent cIAp1-based degrader of cellular retinoic acid binding protein (CRABP-II).
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规格数量 - SNIPER(ABL)-039T186902222354-29-0SNIPER(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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规格数量 - PROTAC ERα Degrader-2T186051351169-29-3PROTAC 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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规格数量 - SNIPER(ABL)-047T18692SNIPER(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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规格数量 - SNIPER(ABL)-024T186882222355-77-1SNIPER(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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规格数量 - SNIPER(ABL)-050T18694SNIPER(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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规格数量 - SNIPER(ABL)-033T186892222354-18-7SNIPER(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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规格数量 - SNIPER(ABL)-019T18686SNIPER(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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规格数量 - SNIPER(ABL)-058T186952222354-61-0SNIPER(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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规格数量 - SNIPER(ER)-110T18696SNIPER(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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规格数量 - SNIPER(ABL)-013T18684SNIPER(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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规格数量 - SNIPER(TACC3)-2T13892SNIPER(TACC3)-2 targets TACC3 protein degradation via the ubiquitin-proteasome pathway. It induces cancer cell death.
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规格数量 - PROTAC RAR Degrader-1T186351351169-27-1PROTAC 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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规格数量 - SNIPER(ABL)-049T18693SNIPER(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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规格数量 - SNIPER(ABL)-044T18691SNIPER(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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规格数量 - SNIPER(TACC3)-1T13891SNIPER(TACC3)-1 targets TACC3 protein degradation via the ubiquitin-proteasome pathway.It induces cancer cell death.
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规格数量 - BzNH-BST17706BzNH-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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规格数量 - SNIPER(ABL)-020T18687SNIPER(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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规格数量 - Biotin-BST17545Biotin-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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规格数量 - PROTAC CRABP-II Degrader-1T138361225383-40-3PROTAC CRABP-II Degrader-1 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on cIAp1.
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规格数量 - SNIPER(BRD)-1T169052095244-54-3SNIPER(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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规格数量 - SNIPER(ER)-87T186972222354-91-6SNIPER(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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规格数量 - PROTAC CRABP-II Degrader-3T138381225383-41-4PROTAC CRABP-II Degrader-3 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on [cIAp1].
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