PROTACs
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PROTACs Related Products (436)
Related Products (436)
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PROTAC EML4-ALK Degrader-1
0 ImagesCat. No.: HY-174368Synonyms: Pro-BAPROTAC EML4-ALK Degrader-1 (Pro-BA) is an orally active EML4-ALK PROTAC degrader that recruits GID4, with a Kd value of 144 nM against human EML4-ALK and a DC50 of 74 nM in H3122 cells. PROTAC EML4-ALK Degrader-1 promotes EML4-ALK ubiquitination and proteasomal degradation, reduces cancer cell viability, inhibits cancer cell and tumor growth, induces apoptosis, and alters cell cycle distribution. PROTAC EML4-ALK Degrader-1 can be used in studies related to EML4-ALK-positive cancers and non-small cell lung cancer.
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Arg-PEG1-Tαsyn
0 ImagesCat. No.: HY-180976Arg-PEG1-Tαsyn is an α-syn PROTAC degrader with a DC50 of 0.28 μM in U251 cells. Arg-PEG1-Tαsyn employs the amino acid arginine (Arg) as the E3 ligase UBR1 ligand and a benzothiazole-aniline variant as the warhead for α-syn. Arg-PEG1-Tαsyn significantly reduces α-syn aggregates and improves the dopaminergic neuronal impairment and the locomotion with safety profile in vivo.Arg-PEG1-Tαsyn shows the high degradation effect in mammalian cells for both wild-type α-syn and the α-syn (A53T) mutant. Arg-PEG1-Tαsyn can be used for Parkinson’s disease research.
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PROTAC EZH2 Degrader-29
0 ImagesCat. No.: HY-181357CAS No.: 3093642-30-6PROTAC EZH2 Degrader-29 (compound 66) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 24.53 μM against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-29 can be used in studies related to diffuse large B-cell lymphoma.
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MS40
0 ImagesCat. No.: HY-148829CAS No.: 2407449-49-2MS40 is a WDR5 PROTAC degrader with a DC50 of 42 nM in MV4;11 MLL-rearranged acute myeloid leukemia (AML) cells. MS40 induces WDR5 degradation dependent on WDR5, CRBN and the proteasome, dissociates the MLL/KMT2A complex from chromatin, reduces H3K4me2 levels, degrades IKZF1/IKZF3, the novel substrates of CRBN, inhibits the transcription of WDR5/MLL and IKZF target genes, and suppresses cancer cell growth. MS40 can be used in the research of MLL-rearranged acute myeloid leukemia, breast cancer, Burkholderia infection and cystic fibrosis-associated bacterial infections.
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PROTAC SHP2 degrader-1
0 ImagesCat. No.: HY-189468CAS No.: 3128784-74-4PROTAC SHP2 degrader-1 is a potent SHP2 PROTAC degrader with a DC50 of 7.406 μM. PROTAC SHP2 degrader-1 recruits DCAF16 E3 ligase to induce ubiquitination and proteasomal degradation of SHP2, thereby inhibiting the RAS/MAPK and PI3K/AKT/mTOR signaling pathways while simultaneously inducing IFN-γ/JAK/STAT1, apoptosis, and cell cycle arrest. PROTAC SHP2 degrader-1 can be used for cancer research.
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PCC16 chloride
0 ImagesCat. No.: HY-169232PCC16 chloride is a dual PROTAC degrader targeting DHHC3 and PD-L1, with a DC50 of 0.103 μM for PD-L1 degradation. PCC16 chloride induces DHHC3 degradation via the ubiquitin-proteasome pathway by recruiting the CRBN E3 ubiquitin ligase (E3 ubiquitin ligase). By targeting DHHC3-which is essential for PD-L1 palmitoylation and membrane stability-PCC16 chloride reduces PD-L1 levels, decreases PD-L1 membrane retention time, and impairs its immunosuppressive function. PCC16 chloride enhances anti-tumor immunity by disrupting PD-L1-mediated immunosuppression. PCC16 chloride can be used in the research of immune checkpoint blockade-resistant cancers.
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PROTAC MLKL Degrader-2
0 ImagesCat. No.: HY-169072CAS No.: 3103327-20-1PROTAC MLKL Degrader-2 is an orally active and highly selective mixed lineage kinase domain-like pseudokinase (MLKL) PROTAC degrader with a DC50 of 0.012 μM. PROTAC MLKL Degrader-2 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, leading to ubiquitination of MLKL and its degradation via a proteasome-dependent pathway. PROTAC MLKL Degrader-2 inhibits necroptosis, reduces ROS production, restores mitochondrial function, and ameliorates lysosomal dysfunction induced by necroptotic stimuli. PROTAC MLKL Degrader-2 degrades MLKL in xenograft mouse models. PROTAC MLKL Degrader-2 can be used in cancer-related research.
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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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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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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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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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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.
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RPG-01-132
0 ImagesCat. No.: HY-181920RPG-01-132 is a PROTAC degrader targeting the DENV capsid protein, with a DC50 of 2.4 μM. RPG-01-132 blocks viral assembly, eliminates viral particles, and interferes with the non-structural functions of the capsid protein. RPG-01-132 exhibits significant antiviral activity against all four DENV serotypes and the ST148 (HY-121663)-resistant DENV2 mutant strain. RPG-01-132 can be applied in studies related to dengue virus infection.
