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
All Product Categories
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PROTACs Related Products (1353)
Related Products (1353)
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Antibodies (1)
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PROTACs Isoform Comparison
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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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PROTAC BRD4 Degrader-50
0 ImagesCat. No.: HY-157426CAS No.: 3093737-33-5
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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 ImagesCat. No.: HY-178360CAS No.: 2966791-41-1NP1192 is a potent, selective PROTAC NAT10 degrader that depletes NAT10 protein and inhibits ac4C modification in cancer cells. 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. (Blue: CRBN ligand (HY-148834); Black: linker; Pink: NAT10 ligand (HY-16706)).
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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 Sirt2 Degrader-2
0 ImagesCat. No.: HY-179388PROTAC Sirt2 Degrader-2 is a highly efficient and selective PROTAC degrader targeting SIRT2. PROTAC Sirt2 Degrader-2 demonstrates the most potent anti-proliferative activity both in vitro and in vivo. PROTAC Sirt2 Degrader-2 leads to a marked increase in H4K16Ac levels. PROTAC Sirt2 Degrader-2 significantly suppresses clonogenic formation and migration, induces cell cycle arrest, and promotes apoptosis. PROTAC Sirt2 Degrader-2 inhibits the AKT/mTOR signaling pathway by indirectly degrading SIRT2 and blocking downstream protein phosphorylation, thereby disrupting the signaling cascade and suppressing tumor development. PROTAC Sirt2 Degrader-2 can be used for the study of ovarian cancer.
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PROTAC TBL1X degrader-1
0 ImagesCat. No.: HY-168190PROTAC TBL1X degrader-1 is a TBL1X PROTAC degrader. PROTAC TBL1X degrader-1 induces TBL1X degradation via the Cereblon-mediated proteasomal pathway. PROTAC TBL1X degrader-1 exerts cytotoxic effects on cancer cells. PROTAC TBL1X degrader-1 can be used in studies related to diffuse large B-cell lymphoma.
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PROTAC CDK9 degrader-13
0 ImagesCat. No.: HY-184693PROTAC CDK9 degrader-13 is a selective CDK9 degrader acting via the ubiquitin-proteasome system. PROTAC CDK9 degrader-13 induces apoptosis in acute myeloid leukemia cells. PROTAC CDK9 degrader-13 suppresses tumor growth in vivo and has a defined safety profile. PROTAC CDK9 degrader-13 can be used for the research of acute myeloid leukemia.
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PROTAC BRD4 Degrader-32
0 ImagesCat. No.: HY-176449PROTAC BRD4 Degrader-32 (Compound 22) is a BRD4 PROTAC degrader (DC50: 0.20 nM). PROTAC BRD4 Degrader-32 connects the BRD4-binding domain and CRBN-binding domain through a unique carbon-carbon linked linker to form a ternary complex, inducing ubiquitination of BRD4 for proteasomal degradation. PROTAC BRD4 Degrader-32 is promising for research of BRD4-related cancers (such as hematological malignancies).
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LWY713
0 ImagesCat. No.: HY-157213LWY713 is a FLT3 PROTAC degrader with a DC50 of 0.64 nM. LWY713 selectively induces FLT3 degradation in a cereblon- and proteasome-dependent manner. LWY713 induces G0/G1 cell cycle arrest and triggers apoptosis. LWY713 upregulates PARP and cleaved caspase 3, and inhibits the phosphorylation of FLT3, STAT5, AKT and Erk. LWY713 exhibits antitumor activity in xenograft mouse models. LWY713 can be used for the research of acute myeloid leukemia.
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PROTAC SMARCA2 degrader-7
0 ImagesCat. No.: HY-159451CAS No.: 2568277-71-2PROTAC SMARCA2 degrader-7 (Compound I-428) is a PROTAC degrader for SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A (SMARCA) SMARCA2. PROTAC SMARCA2 degrader-7 degrades SMARCA2 and SMARCA4 in MV411 with DC50 of <100 and 100-500 nM. (Pink: Ligand for target protein (HY-159542); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
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MS910
0 ImagesCat. No.: HY-170982CAS No.: 2756323-28-9MS910 is an efficient and selective MEK1/2 PROTAC degrader. MS910 exhibits effective MEK1/2 degradation ability and anti proliferative activity in various cancer cells, such as HT-29 (MEK1 DC50 = 118 nM, MEK2 DC50 = 55 nM) and SK-MEL-28 (MEK1 DC50 = 94 nM, MEK2 DC50 = 38 nM) cells. MS910 is commonly used in cancer research. (Pink: MEK1/2 Ligand (HY-10254); Blue: CRBN Ligand (HY-W087383); Black: Linker (HY-W022240))
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DW-229
0 ImagesCat. No.: HY-183618DW-229 is a PROTAC degrader derived from Deferiprone (HY-B0568), targeting Fe(II)/α‑ketoglutarate‑dependent histone lysine demethylases (KDMs). DW-229 degrades KDM2A, KDM3A, KDM5B, KDM4A‑C, KDM5C, KDM6B in breast cancer cells. DW-229 shows IC50 < 0.5 μM against MCF‑7 cells and IC50 of 8.87 μM against MDA‑MB‑231 cells, with high cancer cell selectivity. DW-229 can be used for the research of breast cancer, liver cancer, prostate cancer, lung cancer.
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FKBP12 PROTAC FM4
0 ImagesFKBP12 PROTAC FM4 is a PROTAC degrader of FKBP12, with a DC50 value of 0.09-0.22 nM. FKBP12 PROTAC FM4 inhibits global protein synthesis, induces apoptosis, and selectively reduces the viability of cervical cancer cells expressing MTH1-E6 and FKBP12F36V-tagged SARS1. FKBP12 PROTAC FM4 is applicable to research related to HPV-positive cervical cancer.
