PROTACs
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PROTACs Related Products (454)
Related Products (454)
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INY-05-040
0 ImagesINY-05-040 is an AKT degrader that can selectively and quickly degrade all three AKT isoforms. INY-05-040 exhibits anti-cancer activity. INY-05-040 can inhibit downstream signaling and cell proliferation in 288 cancer cell lines. INY-05-040 can suppress AKT signaling and induces the stress mitogen-activated protein kinase (MAPK) c-Jun N-terminal kinase (JNK). INY-05-040 is effective for breast cancer lines with a low-baseline activation of stress MAPK pathway. INY-05-040 can be studied for anti-cancer research.
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MS21
0 ImagesMS21 is an effective AKT PROTAC degrader. MS21 can inhibit mutations in the PI3K/PTEN pathway, suppress the proliferation and induce cell cycle arrest of tumor cells. MS21 has anti-tumor activity. (Pink: AKT ligand-2 (HY-48682); Black: Linker (HY-W014125); Blue: (S,R,S)-AHPC (HY-125845)).
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ARD-2585
0 ImagesARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
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PROTAC IRAK3 degrade-1 formic
0 ImagesCat. No.: HY-142662APurity: 99.26%
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DAS-5-oCRBN
0 ImagesDAS-5-oCRBN is a PROTAC molecule with both c‑Src kinase inhibitory activity and target protein degradation activity, with an EC50 of 45 nM for c‑Src binding. DAS-5-oCRBN binds non-covalently to Cereblon and mediates target protein degradation via the ubiquitin-proteasome pathway. DAS-5-oCRBN can catalytically deplete intracellular c‑Src protein, while blocking both the kinase catalytic function of c‑Src and the non-catalytic protein interactions mediated by its SH2 and SH3 domains. DAS-5-oCRBN inhibits tumor cell proliferation and exerts significant anti-proliferative effects on both c‑Src kinase activity-dependent MDA-MB-231 cells and c‑Src protein level-dependent CAL51 cells. DAS-5-oCRBN can be used in cancer-related research such as studies on triple-negative breast cancer and chronic myeloid leukemia.
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MS6105
0 ImagesMS6105 is a PROTAC degrader targeting LDHA and LDHB, with DC50 values of 38 nM and 74 nM for degrading LDHA and LDHB in PANC-1 cells, respectively, and no hook effect is observed at high concentrations. MS6105 inhibits the proliferation of pancreatic cancer cells, and no obvious toxicity is observed after intraperitoneal administration in mice. MS6105 can be used for pancreatic cancer-related research.
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BSJ-03-204 triTFA
0 ImagesCat. No.: HY-136250APurity: 99.87%BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 triTFA is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and has anti-cancer activity.
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ARD-2128
0 ImagesARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
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PROTAC KDM3 degrader-1
0 ImagesPROTAC KDM3 degrader-1 is a KDM3A/KDM3B PROTAC degrader with DC50 values of 13.73 nM and 172.6 nM in SW480 cells, respectively. PROTAC KDM3 degrader-1 induces cereblon-dependent proteasomal degradation of KDM3A and KDM3B. PROTAC KDM3 degrader-1 inhibits the oncogenic Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 eliminates colorectal cancer stem cells, suppresses their self-renewal, and blocks colony formation of colorectal cancer cells. PROTAC KDM3 degrader-1 inhibits tumor growth in a colorectal cancer xenograft mouse model. PROTAC KDM3 degrader-1 can be used for the research of colorectal cancer.
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PRO-6E
0 ImagesPRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)).
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GDC-2992
0 ImagesSynonyms: RO7656594GDC-2992 (Compound 28A) is an orally bioavailable androgen receptor (AR) PROTAC degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study.
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PROTAC PTPN2 degrader-1
0 ImagesCat. No.: HY-148691CAS No.: 2655638-07-4PROTAC PTPN2 degrader-1 is a PROTAC degrader targeting non-receptor protein tyrosine phosphatase 2 (PTPN2), with a DC50 of 18 nM in 293T cells. It exhibits an IC50 of 22 nM against PTPN2. Through highly selective degradation and inhibition of PTPN2 phosphatase, PROTAC PTPN2 degrader-1 relieves the negative regulation of the IFNγ pathway, upregulates interferon signaling, activates effector T cells, and enhances anti-tumor immunity. PROTAC PTPN2 degrader-1 can be used in melanoma-related research.
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PROTAC AR Degrader-8
0 ImagesPROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC50s of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 values of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer.
