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 (1386)
Related Products (1386)
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Antibodies (1)
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PROTACs Isoform Comparison
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DT2216 (Standard)
0 ImagesCat. No.: HY-130604RCAS No.: 2365172-42-3DT2216 (Standard) is the analytical standard of DT2216 (HY-130604). This product is intended for research and analytical applications. DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
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dBET6 (Standard)
0 ImagesCat. No.: HY-112588RCAS No.: 1950634-92-0
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CRBN ligand-186
0 ImagesCat. No.: HY-174249CAS No.: 3084710-09-5
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Homo-PROTAC cereblon degrader 1 (Standard)
0 ImagesCat. No.: HY-111594RCAS No.: 2244520-98-5Homo-PROTAC cereblon degrader 1 (Standard) is the analytical standard of Homo-PROTAC cereblon degrader 1 (HY-111594). This product is intended for research and analytical applications. Homo-PROTAC cereblon degrader 1 is a highly selective cereblon (CRBN) PROTAC degrader. Homo-PROTAC cereblon degrader 1 induces self-directed ubiquitination and proteasomal degradation of CRBN. Homo-PROTAC cereblon degrader 1 blocks Pomalidomide (HY-10984)-induced degradation of IKZF1 and IKZF3. Homo-PROTAC cereblon degrader 1 antagonizes the growth inhibitory effect of Pomalidomide on multiple myeloma cells. Homo-PROTAC cereblon degrader 1 can be used in studies related to multiple myeloma.
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PROTAC Sirt2 Degrader-1 (Standard)
0 ImagesCat. No.: HY-103636RCAS No.: 2098487-75-1PROTAC Sirt2 Degrader-1 (Standard) is the analytical standard of PROTAC Sirt2 Degrader-1 (HY-103636). This product is intended for research and analytical applications. PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM).
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BMS-986365 (Standard)
0 ImagesCat. No.: HY-158101RCAS No.: 2446928-30-7Synonyms: CC-94676 (Standard)BMS-986365 (Standard) is the analytical standard of BMS-986365 (HY-158101). This product is intended for research and analytical applications. BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC).
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rG4 WT_AHPC_PEG2
0 ImagesCat. No.: HY-185723rG4 WT_AHPC_PEG2 is a selective RNA G-quadruplex-based DHX36 PROTAC degrader with a Kd value of 79.7 nM. rG4 WT_AHPC_PEG2 degrades DHX36 via a proteasome-dependent mechanism, without significantly degrading other G4-binding proteins including NCL, DHX9, hnRNP, SRSF and FMR1.
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(S)-JNJ-1013
0 ImagesCat. No.: HY-153188ACAS No.: 2755075-91-1(S)-JNJ-1013 is an isomer of IRAK1 PROTAC degrader JNJ-1013 (HY-153188). (S)-JNJ-1013 loses VHL binding affinity (IC50 >10 μM) and shows no significant IRAK1 degradation activity (DC50 > 10 μM). (S)-JNJ-1013 selectively inhibits IRAK1 with an IC50 of 79 nM. (S)-JNJ-1013 can be used to study cancers dependent on the scaffolding function of IRAK1.
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ARV-771 (Standard)
0 ImagesCat. No.: HY-100972RCAS No.: 1949837-12-0ARV-771 (Standard) is the analytical standard of ARV-771 (HY-100972). This product is intended for research and analytical applications. ARV-771 is a BET PROTAC degrader, with Kd values of 34, 4.7, 8.3, 7.6, 9.6 and 7.6 nM against BRD2 (1), BRD2 (2), BRD3 (1), BRD3 (2), BRD4 (1) and BRD4 (2) , respectively. ARV-771 inhibits the transcription of AR/AR-v7 and its downstream target genes. By degrading BRD4 protein, ARV-771 enhances the sensitivity of prostate cancer cells to ferroptosis, suppresses cancer cell viability, and induces apoptosis. ARV-771 downregulates the levels of BRD4, c-MYC and AR-V7 in tumor tissues and inhibits tumor tissue growth. ARV-771 can be used in prostate cancer-related research.
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vRNPs degrader-1
0 ImagesCat. No.: HY-177791vRNPs degrader-1 is a potent PROTAC viral ribonucleoproteins (vRNPs) degrader. vRNPs degrader-1 shows broad-spectrum anti-influenza A viruses (IAV) activity by targeting the conserved 5′ end of viral RNA, thereby inducing proteasomal degradation of viral proteins. vRNPs degrader-1 inhibits H1N1, H9N2, and H3N2 infection in mice. vRNPs degrader-1 can be used for influenza research.
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PROTAC SARS-CoV-2 Mpro degrader-7
0 ImagesCat. No.: HY-181193PROTAC SARS-CoV-2 Mpro degrader-7 is a SARS-CoV-2 main protease (Mpro) PROTAC degrader with a DC50 of 0.985 μM. PROTAC SARS-CoV-2 Mpro degrader-7 promotes K48-linked polyubiquitination of SARS-CoV-2 Mpro, leading to proteasome-dependent degradation via the ubiquitin-proteasome system.PROTAC SARS-CoV-2 Mpro degrader-7 forms a ternary complex with SARS-CoV-2 Mpro and CRBN E3 ubiquitin ligase to enable viral protease ubiquitination.PROTAC SARS-CoV-2 Mpro degrader-7 exhibits a high selectivity index, and induces dose-dependent degradation of SARS-CoV-2 Mpro in stable cells expressing the viral protease.PROTAC SARS-CoV-2 Mpro degrader-7 can be used for the research of COVID-19.
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BI-3663 (Standard)
0 ImagesCat. No.: HY-111546RCAS No.: 2341740-84-7BI-3663 (Standard) is the analytical standard of BI-3663 (HY-111546). This product is intended for research and analytical applications. BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker. Anti-cancer activity.
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PROTAC SARS-CoV-2 Mpro degrader-3
0 ImagesCat. No.: HY-161789PROTAC SARS-CoV-2 Mpro degrader-3 is a SARS-CoV-2 Mpro PROTAC degrader with a DC50 of 27 μM in HEK 293T cells. It also acts as an inhibitor of HCoV-229E, HCoV-OC43 and SARS-CoV-2 Mpro, with an IC50 of 0.748 μM and a Kd of 37 μM against SARS-CoV-2 Mpro. PROTAC SARS-CoV-2 Mpro degrader-3 forms a ternary complex with purified SARS-CoV-2 Mpro and VCB E3 ligase to induce intracellular protease degradation. It reduces coronavirus replication and can be used in research on coronavirus infections.
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PROTAC SARS-CoV-2 Mpro degrader-8
0 ImagesCat. No.: HY-181870PROTAC SARS-CoV-2 Mpro degrader-8 is an antiviral PROTAC degrader targeting the SARS-CoV-2 main protease (Mpro), with weak direct binding affinity to Mpro (Kd=80.5 μM). PROTAC SARS-CoV-2 Mpro degrader-8 exhibits broad-spectrum antiviral activity against SARS-CoV-2 and the human endemic coronavirus HCoV-OC43. It can be used for research on coronavirus infections.
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PROTAC DHFR Degrader-1
0 ImagesCat. No.: HY-181813CAS No.: 3077918-47-6PROTAC DHFR Degrader-1 is a selective PROTAC degrader targeting Plasmodium falciparum DHFR-TS with a Ki of 2.01 nM. PROTAC DHFR Degrader-1 exhibits no inhibitory activity against human DHFR and suppresses the growth of Plasmodium falciparum. PROTAC DHFR Degrader-1 can be used for the research of Plasmodium falciparum and malaria.
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rG4 mut_AHPC_PEG2
0 ImagesCat. No.: HY-185724rG4 mut_AHPC_PEG2 is a structure-disruptive negative control PROTAC. rG4 mut_AHPC_PEG2 demonstrates that the RNA G-quadruplex conformation is an absolute prerequisite for the recruitment and degradation of DHX36 by retaining the E3-recruiting moiety (AHPC-PEG2) while disrupting the secondary structure of the nucleic acid moiety (mutated RNA G-quadruplex),.
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PROTAC HIV-1 degrader-1
0 ImagesCat. No.: HY-187361CAS No.: 3107740-33-7PROTAC HIV-1 degrader-1 is a HIV-1 capsid (CA) PROTAC degrader, with a DC50 of 3 nM against HIV-1IIIB (MT‑4 cells) and a DC50 of 1.17 nM against HIV-1NL4-3 (MT‑4 cells). PROTAC HIV-1 degrader-1 conjugates HIV-1 capsid (CA) with the VHL E3 ubiquitin ligase, triggering polyubiquitination and proteasome-mediated degradation of CA, as well as competitively inhibiting the binding of host factors CPSF6 and Sec24C to CA. PROTAC HIV-1 degrader-1 degrades CA drug-resistant mutants (N74D, K70R). PROTAC HIV-1 degrader-1 is applicable to research related to HIV-1 infection.
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Vepdegestrant (Standard)
0 ImagesCat. No.: HY-138642RCAS No.: 2229711-68-4Synonyms: ARV-471 (Standard); PF-07850327 (Standard)Vepdegestrant (Standard) is the analytical standard of Vepdegestrant (HY-138642). This product is intended for research and analytical applications. Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM.
