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 (1390)
Related Products (1390)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC D16-M1P2
0 ImagesCat. No.: HY-180485PROTAC D16-M1P2 is an orally active CRBN-mediated selective PKMYT1 PROTAC degrader, with a DC50 of 0.7 nM in CCNE1-amplified HCC1569 breast cancer cells. PROTAC D16-M1P2 induces PKMYT1 degradation via the ubiquitin-proteasome system, directly inhibits PKMYT1 kinase activity, suppresses Thr14 phosphorylation of CDK1, and depends on functional CRBN and ubiquitination-like modification processes. PROTAC D16-M1P2 can be used for the research of CCNE1-amplified breast cancer, FBXW7-mutated cholangiocarcinoma, and PPP2R1A-deficient cancers.
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PROTAC BLIMP-1 degrader-1
0 ImagesCat. No.: HY-180177Purity: 98.49%PROTAC BLIMP-1 degrader-1 is an orally active BLIMP-1 PROTAC degrader with an EC50 of 13.1 nM. PROTAC BLIMP-1 degrader-1 recruits the neprilysin (CRBN) E3 ligase to mediate ubiquitination and subsequent degradation of BLIMP-1α via the 26S proteasome, without affecting the BLIMP-1β isoform. PROTAC BLIMP-1 degrader-1 inhibits cancer cell proliferation and tumor growth. It can be used in research related to multiple myeloma.
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MS9427
0 ImagesCat. No.: HY-147941CAS No.: 2772613-37-1MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer.
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PROTAC BCL6 Degrader-2
0 ImagesCat. No.: HY-178803Purity: 99.70%PROTAC BCL6 Degrader-2 is an orally active, selective BCL6 PROTAC degrader (DC50: 0.45 nM in HEK293T cells). PROTAC BCL6 Degrader-2 promotes ubiquitination and degradation of BCL6. It exhibits anticancer activity against BCL6-dependent diffuse large B-cell lymphoma. PROTAC BCL6 Degrader-2 can be used for the research of diffuse large B-cell lymphoma.
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TO-1187
0 ImagesCat. No.: HY-173266TO-1187 is a selective HDAC6 PROTAC degrader with a DC50 value of 5.81 nM. TO-1187 degrades HDAC6 via the ubiquitin-proteasome pathway. TO-1187 can be used in the research of multiple myeloma, neuroblastoma, and cervical cancer.
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AA-BR-157
0 ImagesCat. No.: HY-168969AA-BR-157 is a metallothionein 2A (MT2A) PROTAC degrader, DC50 is 200 nM (MT2A overexpressed in MDA-MB-231 cells). AA-BR-157 increases intracellular zinc levels, downregulates DIAPH3, disrupts cytoskeleton remodeling, and reduces the migration and invasion abilities of cancer cells. AA-BR-157 can be used for research on triple-negative breast cancer and glioblastoma.
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DeFer-2
0 ImagesDeFer-2 is a Ferritin PROTAC degrader with a Kd value of 17.1 μM. DeFer-2 recruits the VHL E3 ligase to induce targeted degradation of ferritin via the ubiquitin-proteasome system, triggers iron overload stress in cancer cells, and further activates caspase 3-GSDME-mediated pyroptosis through massive ROS production. DeFer-2 can be used for research related to melanoma.
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G9D-4
0 ImagesCat. No.: HY-162749CAS No.: 3097803-96-5G9D-4 is a G9a PROTAC degrader. G9D-4 induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 can be used for research on pancreatic cancer.
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NU227326
0 ImagesCat. No.: HY-173066CAS No.: 3048196-52-4NU227326 is a blood-brain barrier penetrant IDO1 PROTAC degrader, with a DC50 of 4.5 nM in HiBiT degradation assays. NU227326 degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively (WB assays). NU227326 is applicable to research related to glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer.
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PROTAC HDAC6 degrader 7
0 ImagesCat. No.: HY-179421PROTAC HDAC6 degrader 7 is an orally active, highly efficient, and selective PROTAC degrader targeting histone deacetylase 6 (HDAC6) (IC50 = 118 nM). PROTAC HDAC6 degrader 7 can eliminate both the catalytic and zinc-finger ubiquitin-binding domain. PROTAC HDAC6 degrader 7 inhibits NLRP3 inflammasome assembly and activation, as well as blocks NF-κB signaling, thereby reducing the transcription and release of key inflammatory factors. PROTAC HDAC6 degrader 7 can reduce the mRNA levels of NLRP3, pro-IL-1β, TNF-α, and IL-6. PROTAC HDAC6 degrader 7 can be used for the study of inflammatory bowel disease (IBD).
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JB300
0 ImagesJB300 is a PROTAC degrader that selectively targets and degrades AURORA-A by recruiting cereblon, with EC50 values of 373 nM and 193 nM in intact cells and permeabilized cells, respectively. JB300 can be used in studies related to acute myeloid leukemia and targeted protein degradation mechanisms.
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YZ-836P
0 ImagesCat. No.: HY-182820CAS No.: 3086041-35-9YZ-836P is a Protein arginine methyltransferase 5 (PRMT5) targeting agent. YZ-836P promotes ubiquitination and proteasomal degradation of PRMT5 in a cereblon (CRBN)-dependent manner, which in turn reduces levels of its downstream target KLF5. YZ-836P induces G1 phase cell cycle arrest in triple-negative breast cancer cells. YZ-836P induces Apoptosis in triple-negative breast cancer cells. YZ-836P exerts cytotoxic effects on triple-negative breast cancer cells. YZ-836P inhibits the growth of triple-negative breast cancer patient-derived organoids. YZ-836P inhibits the growth of triple-negative breast cancer xenografts in nude mice. YZ-836P can be used for the research of triple-negative breast cancer.
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XY-06-007
0 ImagesXY-06-007 is a mutation-selective PROTAC degrader targeting BRD4BD1L94V, with a DC50, 6 h of 10.2 nM in Flp293T cells. XY-06-007 recruits the E3 ligase CRL4CRBN to BRD4BD1L94V, triggering ubiquitination and proteasomal degradation. XY-06-007 can be combined with the dTAG strategy to achieve degrader-mediated synchronous depletion of the corresponding protein fusion in cells. XY-06-007 is applicable for cancer research.
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DU-14 (PTP1B/TC-PTP PROTAC)
0 ImagesDU-14 (PTP1B/TC-PTP PROTAC) is a potent and selective PTP1B and TC-PTP dual PROTAC degrader. DU-14 (PTP1B/TC-PTP PROTAC) has the IC50 for PTP1B and TC-PTP phosphatase activity of 24.2 nM and 30.1 nM, respectively. DU-14 (PTP1B/TC-PTP PROTAC) enhances IFN-γ signaling, promotes T cell activation, and has anti-tumor activity.
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SJFδ
0 ImagesCat. No.: HY-114405CAS No.: 2254609-23-7SJFδ is a p38δ PROTAC degrader with a DC50 of 46.17 nM. SJFδ selectively induces ubiquitin-proteasome-dependent degradation of p38δ by forming a ternary complex with p38δ and the VHL E3 ligase, with no effect on other p38 isoforms or members of the MAPK family. SJFδ can be used for breast cancer research.
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PROTAC FGFR2 degrader 1
0 ImagesCat. No.: HY-163985CAS No.: 3099123-99-3PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model.
