Hsp-targeting Chimeras
HspTACs
Hsp-targeting Chimeras (HspTACs) represent a small-molecule targeted protein degradation platform based on heat shock proteins (Hsp). By conjugating a ligand for a protein of interest (POI) with an Hsp ligand, HspTACs harness the chaperone function of Hsp to mediate protein degradation via either the ubiquitin-proteasome system or the endosomal-lysosomal pathway. Furthermore, HspTACs capitalize on the characteristic overexpression of Hsp70 or Hsp90 in tumor cells; this feature promotes their preferential accumulation within these cells, thereby enabling tumor-selective degradation of the target protein (POI) specifically within Hsp-abundant tumor cells.
Hsp-targeting Chimeras Isoform Specific Products
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Hsp-targeting Chimeras Related Products (8)
Related Products (8)
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Hsp-targeting Chimeras Isoform Comparison
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HEMTAC CDK4/6 degrader 1
0 ImagesHEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer. HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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HEMTAC WEE1 degrader-1
0 ImagesHEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker).
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AurAP14
0 ImagesAurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 can form a stable ternary complex with Aurora A kinase and HSP90, recruiting cullin family E3 ubiquitin ligases and MDM2 to mediate the ubiquitination and proteasome degradation of Aurora A kinase. AurAP14 increases p53 levels and decreases C-MYC levels; AurAP14 induces Apoptosis. AurAP14 can be used in the study of non-small cell lung cancer.
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DDO3602
0 ImagesCat. No.: HY-178496DDO3602 is a PARP1 HSPTAC (HSP90-mediated proteolysis-targeting chimera) degrader, with a DC50 of 490.3 nM against PARP1; its Kd values for PARP1 and HSP90 are 66.5 nM and 1.64 nM, respectively. DDO3602 induces the formation of an unnatural PARP1-HSP90 ternary complex, recruits E3 ubiquitin ligase, and promotes PARP1 degradation via the ubiquitin-proteasome pathway. DDO3602 induces G2/M cell cycle arrest, DNA damage, inhibits cell migration, and exhibits antiproliferative activity in breast cancer cells. DDO3602 can be used in breast cancer-related research.
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AR/AR-V7 degrader-1
0 ImagesCat. No.: HY-181727AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer.
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HEMTAC AR degrader-1
0 ImagesCat. No.: HY-187229HEMTAC AR degrader-1 is an androgen receptor (AR) HEMTAC degrader that recruits HSP70, with a Kd value of 825 nM for HSP72. HEMTAC AR degrader-1 induces AR degradation, and inhibits the proliferation and migration of cancer cells. HEMTAC AR degrader-1 can be used in the research of prostate cancer.
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Hsp70TAC PD-1 Degrader-2
0 ImagesCat. No.: HY-182959Hsp70TAC PD-1 Degrader-2 is a PD-L1 Hsp70TAC (Hsp70-targeting Chimeras) degrader with Kd values of 0.36 μM. Hsp70TAC PD-1 Degrader-2 forms a ternary complex with Hsp70 and PD-L1 to drive PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 induces degradation of mature membrane-bound PD-L1 in an Hsp70-dependent manner and via caveolin-mediated endocytosis and lysosomal trafficking. Hsp70TAC PD-1 Degrader-2 accumulates preferentially in tumor cells with elevated Hsp70 expression for tumor-selective PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 can be used for the research of cancer, such as breast invasive carcinoma, glioblastoma multiforme, diffuse large b-cell lymphoma. (Pink: PD-1/PD-L1 ligand (HY-19745A); Blue: Hsp70 ligand (HY-182979); Black: linker (HY-182982)).
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Hsp70TAC BRD4 Degrader-1
0 ImagesCat. No.: HY-182958Hsp70TAC BRD4 Degrader-1 is a degrader targeting BRD4, with a KD value of 0.22 μM. Hsp70TAC BRD4 Degrader-1 forms a ternary complex with Hsp70 (KD: 5.13 μM), and specifically and efficiently degrades intracellular BRD4 via the ubiquitin-proteasome pathway. Hsp70TAC BRD4 Degrader-1 exhibits potent anti-tumor proliferative activity. Hsp70TAC BRD4 Degrader-1 can be used in studies related to triple-negative breast cancer and glioblastoma multiforme. (Pink: BRD4 ligand (HY-78695); Blue: HSP70 ligand (HY-182979); Black: linker (HY-B0236)).
