PROTACs
PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.
PROTACs Isoform Specific Products
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PROTACs Related Products (1398)
Related Products (1398)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC SOS1 degrader-6
0 ImagesCat. No.: HY-162281CAS No.: 3032282-51-9PROTAC SOS1 degrader-6 is a selective SOS1 PROTAC degrader with a DC50 of 43-130 nM. PROTAC SOS1 degrader-6 induces ubiquitination and degradation of SOS1 via the ubiquitin-proteasome system by recruiting the E3 ligase VHL. PROTAC SOS1 degrader-6 reduces the levels of phosphorylated MEK and ERK. PROTAC SOS1 degrader-6 exerts antiproliferative effects in KRAS-driven cancer cells. PROTAC SOS1 degrader-6 can be used in research related to KRASG12C-mutant cancers and chronic myeloid leukemia.
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SK4454
0 ImagesCat. No.: HY-179640SK4454 is a selective AURKA PROTAC degrader degrading AURKA with IC50 = 8 nM. MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK4454 efficiently reduced AURKA levels in vivo. SK4454 can be used for neuroblastoma research.
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PROTAC Hemagglutinin Degrader-1
0 ImagesCat. No.: HY-147654CAS No.: 3031330-66-9PROTAC Hemagglutinin Degrader-1 (Compound V3) is a potent PROTAC influenza hemagglutinin (HA) degrader with a median degradation concentration of 1.44 μM. PROTAC Hemagglutinin Degrader-1 shows broad-spectrum anti-influenza virus activity.
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PROTAC ALK degrader-2
0 ImagesCat. No.: HY-161750PROTAC ALK degrader-2 (B1-PEG) is an ALK degrader based on PROTACs, with the DC50 of 45 nM in H3122 EML4-ALK DC50 (GSH+). PROTAC ALK degrader-2, through PEGylation, is engineered to self-organize into micelles in water and releases its active form in response to the tumor-specific high GSH environment.
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TD-802
0 ImagesCat. No.: HY-146397CAS No.: 2760703-21-5TD-802 is a CRBN-recruiting PROTAC androgen receptor (AR) degrader with liver microsomal stability and in vivo pharmacokinetic properties. TD-802 exhibits weak degrading activity against the AR-V7 splice variant, and its degradation process depends on the ubiquitin-proteasome system and Cullin-Ring ubiquitin ligase. TD-802 inhibits the proliferation of AR-dependent prostate cancer cells and the growth of AR-positive prostate cancer tumors in in vivo xenograft models.
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LGF308
0 ImagesCat. No.: HY-181756CAS No.: 3061406-69-4LGF308 is a PROTAC degrader of BRD4 that exhibits selective cytotoxicity toward cancer cells over normal cells. LGF308 mediates the formation of a ternary complex between BRD4 and DCAF11 to achieve BRD4 degradation. LGF308 induces tumor cell apoptosis by upregulating apoptosis-related proteins. LGF308 inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines. LGF308 can be used for the research of breast cancer.
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PROTAC SMARCA2/4 degrader-35
0 ImagesCat. No.: HY-168225CAS No.: 2933253-85-9PROTAC SMARCA2/4-degrader-35 (Ex.43) is a SMARCA2/4 degrader with a DC50 <2.5 nM
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PROTAC TEAD1/IAP degrader-3
0 ImagesCat. No.: HY-181590PROTAC TEAD1/IAP degrader-3 is a TEAD1/IAP PROTAC degrader. PROTAC TEAD1/IAP degrader-3 recruits the cIAP1 and XIAP E3 ligases to form a ternary complex, drives proteasomal degradation of TEAD1, and triggers autoubiquitination and proteasomal degradation of cIAP1. PROTAC TEAD1/IAP degrader-3 inhibits cell proliferation. PROTAC TEAD1/IAP degrader-3 regulates Hippo pathway activity by downregulating CTGF gene expression in a TEAD-dependent manner. PROTAC TEAD1/IAP degrader-3 is applicable to the research of mesothelioma.
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APH003
0 ImagesCat. No.: HY-184915CAS No.: 3065495-08-8APH003 is an orally active IRAK4 PROTAC degrader with a DC50 of 0.74 nM in human peripheral blood mononuclear cells (hPBMCs). APH003 recruits IRAK4 to CRBN to form a ternary complex, mediates the ubiquitination and degradation of IRAK4 via the ubiquitin-proteasome pathway, and inhibits the kinase activity of IRAK4. APH003 inhibits LPS- or IL-1β/LPS-induced phosphorylation of ERK, JNK and NF-κB. APH003 inhibits the secretion of TNF-α, IL-6, IL-8 and IL-13 by stimulated hPBMCs. APH003 exhibits anti-inflammatory activity in rat TNBS-induced intestinal inflammation models and mouse IL-33-induced skin inflammation models. APH003 can be used in research related to inflammatory bowel disease and skin inflammation.
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LO-3-62
0 ImagesCat. No.: HY-175186LO-3-62 is a SMARCA2/4 degrader. LO-3-62 incorporates a truncated fumaramide linker and conjugates it to a SMARCA2/4 inhibitor. LO-3-62 binds covalently to the CUL4DCAF16 E3 ubiquitin ligase, inducing proteasome-dependent degradation of SMARCA2/4. LO-3-62 can be used in studies of monocytic leukemia.
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dCASP1-55
0 ImagesCat. No.: HY-181132dCASP1-55 is a cereblon-dependent caspase-1 (CASP1) PROTAC degrader. dCASP1-55 induces excessive NF-κB activation, apoptosis, and moderate S-phase arrest in leukemic cells. dCASP1-55 suppresses colony formation of leukemic cells. dCASP1-55 can be used for the research of cancer, such as myeloid malignancies and acute myeloid leukemia.
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PROTAC BRD4 Degrader-37
0 ImagesCat. No.: HY-175225PROTAC BRD4 Degrader-37 is a BRD4 PROTAC degrader with a DC50 of 36.4 nM. PROTAC BRD4 Degrader-37 recruits the E3 ubiquitin ligase TRIM21, binds to the PRYSPRY domain of TRIM21 (KD = 123 nM), and thereby mediates the ubiquitination and degradation of BRD4. PROTAC BRD4 Degrader-37 exhibits cytotoxicity against PANC-1 cells (GI50 = 0.282 μM). PROTAC BRD4 Degrader-37 can be used in studies related to pancreatic cancer.
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NP1192
0 ImagesNP1192 is a potent, selective PROTAC NAT10 degrader. NP1192 promotes NAT10 ubiquitination and degradation. NP1192 inhibits ac4C modification. NP1192 demonstrates dual inhibition of hypoxia-driven glycolysis and immunosuppression via NAT10/HIF-1α/PD-L1 axis disruption, achieving superior antitumor efficacy and synergizing with anti-PD-L1 both in vitro and in vivo. NP1192 can be used for ovarian, cervical, and glioblastoma cancer research.
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PROTAC AURKA degrader-4
0 ImagesCat. No.: HY-187470CAS No.: 3135155-78-8PROTAC AURKA degrader-4 is a AURKA PROTAC degrader with a DC50 of 25.62 nM (Jurkat cells). PROTAC AURKA degrader-4 recruits the CRBN E3 ubiquitin ligase via the ubiquitin-proteasome system. PROTAC AURKA degrader-4 disrupts both the catalytic and non-catalytic functions of AURKA, including its interactions with TPX2 and c-Myc. PROTAC AURKA degrader-4 induces G2/M phase arrest and apoptosis. PROTAC AURKA degrader-4 exhibits enhanced antiproliferative activity and in vivo antitumor efficacy in models with high CRBN and AURKA expression. PROTAC AURKA degrader-4 can be used for the research of acute lymphoblastic leukemia.
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PROTAC SMARCA2 degrader-31
0 ImagesCat. No.: HY-168234CAS No.: 2380274-45-1PROTAC SMARCA2-degrader-36 is a PROTAC degrader of SMARCA2, achieving a 99% degradation rate in H929 cells. It also exhibits degradative activity against SMARCA4, but with relatively weaker efficacy. PROTAC SMARCA2-degrader-36 can inhibit cancer cell proliferation and may be used in research related to multiple myeloma.
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PROTAC BCR-ABL Degrader-2
0 ImagesCat. No.: HY-180967CAS No.: 2703834-25-5PROTAC BCR-ABL Degrader-2 is a selective Bcr-AblT315 PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research.
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PROTAC CDK4/6 degrader-2
0 ImagesCat. No.: HY-189460CAS No.: 3135520-67-8PROTAC CDK4/6 degrader-2 is an orally active and selective PROTAC degrader that targets CDK4/6 degradation by recruiting cereblon. PROTAC CDK4/6 degrader-2 exhibits DC50 values of 10.9 nM and 9.6 nM for CDK4 and CDK6, respectively. PROTAC CDK4/6 degrader-2 inhibits RB phosphorylation and cell cycle progression. PROTAC CDK4/6 degrader-2 is applicable for research on breast cancer and CDK4/6 inhibitor resistance.
