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 (1323)
Related Products (1323)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC AR Degrader-9
0 ImagesCat. No.: HY-170448PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for androgen receptor, that degrades AR in human hair follicle papilla cells (HDPCs) with a DC50 of 262.38 nM. PROTAC AR Degrader-9 promotes the expressions of paracrine factors, such as TGF-β1 and β-catenin, exhibits hair regenerating efficacy in mouse models.
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PROTAC ERα Degrader-12
0 ImagesCat. No.: HY-174453PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer.
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PROTAC c-Met degrader-6
0 ImagesCat. No.: HY-175321PROTAC c-Met degrader-6 is a potent and orally active c-Met PROTACdegrader. PROTAC c-Met degrader-6 significantly induces the degradation of the c-Met protein with DC50s of 0.52 nM and 0.45 nM in EBC-1 and Hs746T. PROTAC c-Met degrader-6 almost abrogates the migratory and invasion abilities of tumor cells and significantly induces the apoptosis and blocks the cell cycle in the G0/G1 phase. PROTAC c-Met degrader-6 can be used for the study of various cancers such as non-small cell lung cancer and stomach cancer.
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Naph-Se-TMZ
0 ImagesCat. No.: HY-169433Naph-Se-TMZ is a PROTAC-like HDAC1 degrader. Naph-Se-TMZ induces ROS-dependent reduction in HDAC1 protein expression and total HDAC activity, and decreases cell viability in a dose-dependent manner. Naph-Se-TMZ exhibits activity in both TMZ-sensitive and TMZ-resistant glioma cells, and its cytotoxicity is reversed by the ROS scavenger N-acetylcysteine (HY-B0215). Naph-Se-TMZ can be used in studies related to glioblastoma.
Naph-Se-TMZ consists of a target protein ligand (red segment): Temozolomide (HY-17364), a DNA intercalator (blue segment): Nitro-Naphthalimide-C2-acylamide (HY-169437), and a molecular linker (black segment). Meanwhile, the activity control for the target protein ligand is Temozolomide-amino hydrochloride (HY-169439), and the DNA intercalator+linker is NNISC-2 (HY-169438).
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dTAGV-1-NEG TFA
0 ImagesCat. No.: HY-145514BdTAGV-1-NEG TFA is an inactive FKBP12F36V PROTAC degrader, the diastereomer of dTAGV-1 (HY-145514D), and a heterobifunctional negative control molecule. dTAGV-1-NEG TFA does not degrade any protein.
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PROTAC BRD4 Degrader-38
0 ImagesCat. No.: HY-175240PROTAC BRD4 Degrader-38 is a BRD4 PROTAC degrader with DC50s of 86 and 106 nM for the short and long isoforms of BRD4, respectively. PROTAC BRD4 Degrader-38 significantly induces the degradation of BRD4 by covalently engaging C232 of E3 ligase TRIM28.Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-203082); Black: linker (HY-40172)
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PROTAC AR/BET protein degrader-1
0 ImagesCat. No.: HY-160262CAS No.: 2571123-81-2PROTAC AR/BET protein degrader-1 (Compound 149) is an Androgen Receptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research.
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NEP162
0 ImagesCat. No.: HY-174996CAS No.: 3031840-36-2NEP162 is a BRD4 PROTAC degrader with DC50s of 1.2 and 1.6 μM in SW480 and U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibits tumor growth and induces apoptosis. NEP162 can be used for the study of osteosarcoma, colorectal cancer and non-small cell lung cancer, etc. (Pink: BRD4 ligand : (HY-78695), Blue: E3 ligase Ligand (HY-D2259), BLACK: Linker, E3 ligase ligand-linker conjugate (HY-174997)).
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LHF418
0 ImagesCat. No.: HY-161450LHF418 is an effective SOS1 PROTAC degrader with a DC50 value of 209.4 nM in A549 cells. LHF418 can effectively inhibit RAS signaling and colony formation in KRAS-driven cancer cells. (Structural note: (Blue: Cereblon ligand (HY-A0003), Black: linker; Pink: SOS1 binder SOS1 Ligand intermediate-3 (HY-161452)).
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IBA-12
0 ImagesCat. No.: HY-182799IBA-12 is a IKZF2 molecular glue/PROTAC degrader with a DC50 of 276.2 nM (Jurkat cells) and 461.8 nM (Mino cells), and an IC50 of 179.9 nM. IBA-12 binds to the canonical tryptophan triad pocket of CRBN to form a ternary complex with IKZF2. IBA-12 induces IKZF2 degradation mediated by the CRBN-dependent ubiquitin-proteasome system, with no effect on other CRBN substrates. IBA-12 induces the production of interleukin-2 (IL-2) through degrading IKZF2. IBA-12 is applicable to cancer immunology research.
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PROTAC BcI-2/BcI-xI Degrader-1
0 ImagesCat. No.: HY-158551CAS No.: 3034200-49-9PROTAC Bcl-2/Bcl-xL Degrader-1 is a Bcl-2/Bcl-xL PROTAC degrader with a DC50 of 11.28 nM against Bcl-xL. PROTAC Bcl-2/Bcl-xL Degrader-1 promotes ubiquitination and degradation of Bcl-2/Bcl-xL. It exhibits anticancer activity against acute lymphoblastic leukemia. PROTAC Bcl-2/Bcl-xL Degrader-1 can be used in the research of BCL-2-mediated or BCL-2-dependent diseases.
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HL435
0 ImagesCat. No.: HY-161769HL435 is a BRD4 PROTAC degrader with DC50 values of 11.9 nM (MDA-MB-231 cells) and 21.9 nM (MCF-7 cells), respectively. HL435 recruits the CRL4DCAF11 E3 ubiquitin ligase complex to degrade BRD4 via the ubiquitin-proteasome system. HL435 induces cell cycle arrest and apoptosis (apoptosis) in cancer cells, downregulates the expression levels of cyclin D1 and cyclin B1, activates caspase-9, and induces PARP1 cleavage. HL435 exerts anti-tumor activity both in vitro and in mouse xenograft tumor models. HL435 can be used for the research of breast cancer and prostate cancer.
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SIAIS117
0 ImagesCat. No.: HY-146022CAS No.: 2353494-84-3SIAIS117 is an ALK PROTAC degrader constructed based on Brigatinib (HY-12857) and VHL-1. SIAIS117 exhibits activity not only against wild-type ALK fusion proteins, but also effectively degrades the highly drug-resistant ALK G1202R mutant fusion protein. SIAIS117 significantly inhibits the proliferation of non-small cell lung cancer, small cell lung cancer, anaplastic large cell lymphoma, and drug-resistant cells expressing EML4-ALK G1202R. SIAIS117 can be used in relevant research on the above-mentioned malignant tumors.
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PROTAC CBP/P300 Degrader-4
0 ImagesCat. No.: HY-183802PROTAC CBP/P300 Degrader-4 is a p300/CBP PROTAC degrader with DC50 of 17.4 nM and 10.2 nM against p300 and CBP in U2OS cells, respectively. PROTAC CBP/P300 Degrader-4 forms ternary complexes with p300 or CBP and an E3 ligase, drives ubiquitination, and mediates proteasomal degradation. PROTAC CBP/P300 Degrader-4 can be used for the research of hematological malignancies.
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PROTAC BRD9 Degrader-11
0 ImagesCat. No.: HY-181951PROTAC BRD9 Degrader-11 is a VHL-based BRD9 PROTAC degraderwith an IC50 of 0.66 μM. PROTAC BRD9 Degrader-11 induces selective, proteasome-dependent degradation of BRD9 via the ubiquitin-proteasome system. PROTAC BRD9 Degrader-11 impairs cell viability, suppresses proliferation, and arrests growth of acute myeloid leukemia cells. PROTAC BRD9 Degrader-11 can be used for the research of acute myeloid leukemia.
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PROTAC NAMPT Degrader-28
0 ImagesCat. No.: HY-181880PROTAC NAMPT Degrader-28 is a NAMPT PROTAC degrader with DC50 values of 45 nM and 55 nM in MCF7 and 4T1cl5 cells, respectively. PROTAC NAMPT Degrader-28 retains nicotinamide phosphoribosyltransferase inhibitory activity and does not induce degradation of this enzyme. PROTAC NAMPT Degrader-28 can be used in breast cancer-related research.
