Search Result
Results for "
MG degrader 2
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-152154
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PROTACs
NAMPT
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Cancer
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Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC50 of 41.9 nM. Nampt degrader-2 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). Nampt degrader-2 leads to significant reduction of NAD + and exerts potent antitumor activities .
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- HY-155102
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PROTACs
Glutaminase
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Cancer
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PROTAC TG2 degrader-2 (compound 7) is a selective, competitive degrader targeting Transglutaminase 2 (TG2), with Kd > 100 μM. PROTAC TG2 degrader-2 inhibits the cell migration and decreases the level of TG2 in ovarian cancer cells. PROTAC TG2 degrader-2 can be used for ovarian cancer study .
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- HY-177725
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Molecular Glues
PI4K
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Cancer
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MG degrader 2 (Compound CM-2) is a CRBN-dependent molecular glue degrader. MG degrader 2 induces ZFP91, FIZ1 and PI4KB degradation. MG degrader 2 has anti-proliferative activity against MM.1S cells (IC50 = 162 nM). MG degrader 2 can be used for the research of cancer, such as multiple myeloma .
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- HY-178161
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HDAC
Apoptosis
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Cancer
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HDAC degrader-2 is a selective HDAC degrader with a DC50 values of 2.55 μM against HDAC1. HDAC degrader-2 effectively induces the degradation of HDAC1 and HDAC2, but has no significant effect on the degradation of HDAC3, 4, 6 and 8. HDAC degrader-2 exerts potent antiproliferative effects against MM.1S and MCF-7 cells. HDAC degrader-2 induces apoptosis in myeloma cells. HDAC degrader-2 can be used for the study of myeloma .
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- HY-122828
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PROTACs
Btk
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Others
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PROTAC BTK Degrader-2 is a potent BTK PROTAC degrader. PROTAC BTK Degrader-2 effectively reduces BTK protein levels .
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- HY-177559
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NEKs
Interleukin Related
NOD-like Receptor (NLR)
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Inflammation/Immunology
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NEK7 degrader-2 (Compound 25) is a NEK7 degrader. NEK7 degrader-2 shows dose-dependent NEK7 degradation ability in human PBMC-derived macrophages. NEK7 degrader-2 reduce the release level of pro-inflammatory cytokines IL-1β induced by NLRP3 inflammasome activation. NEK7 degrader-2 can be used for the study of inflammatory diseases .
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- HY-177720
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Molecular Glues
CaMK
Apoptosis
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Cancer
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eEF2K degrader-2 is a molecular glucose degrading agent that targets the eEF2K protein. eEF2K degrader-2 can significantly inhibit the proliferation, migration, invasion and induce apoptosis of triple negative breast cancer (TNBC) cells. eEF2K degrader-2 has no obvious organ toxicity or pathological damage. eEF2K degrader-2 can be used in the research of cancer such as breast cancer .
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- HY-175463
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Molecular Glues
Src
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Cancer
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LCK degrader-2 (Compound 17) is a Lck Molecular glue degrader. LCK degrader-2 can be used for cancers like acute lymphoblastic leukemia (ALL) research .
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- HY-174444A
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PROTACs
HDAC
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Cancer
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PROTAC HDAC degrader-2 TFA is the trifluoroacetate salt of PROTAC HDAC degrader-2. PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC50s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs. ( Pink: HDAC ligand : (HY-174471), Blue: E3 ligase CRBN Ligand (HY-131717), E3 ligase ligand-linker conjugate (HY-174473)) .
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- HY-156747
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Molecular Glues
DNA/RNA Synthesis
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Cancer
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GSPT1 degrader-2 (Compound 210) is a potent and orally active GSPT1 molecular glue degrader (DC50: < 30 nM). GSPT1 degrader-2 is an antitumor agent .
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- HY-163809
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- HY-162544
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PROTACs
MAP4K
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Cancer
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PROTAC HPK1 Degrader-2 (compound 3) is a PROTAC degrader of HPK1, with the DC50 of 23 nM in human PBMC. PROTAC HPK1 Degrader-2 plays an important role in cancer research .
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- HY-168624
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Molecular Glues
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Inflammation/Immunology
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VAV1 degrader-2 (Example 176) is a molecular glue degrader based on targeting VAV 1 with a DC50 of 4.41 nM. VAV1 degrader-2 can be used in the study of inflammatory and autoimmune diseases .
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- HY-162106
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Ferroptosis
PROTACs
Glutathione Peroxidase
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Cancer
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PROTAC GPX4 degrader-2 (compound 18a) is a proteolysis targeting chimeras (PROTACs) that can degrade glutathione peroxidase 4 (GPX4), with the DC50, 48h value of 1.68 μM. PROTAC GPX4 degrader-2 induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. PROTAC GPX4 degrader-2 has anti-proliferative effect .
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- HY-135382
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PROTACs
IRAK
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Inflammation/Immunology
Cancer
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PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC50 in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC50 of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs .
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- HY-128841
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PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
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Cancer
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PROTAC MDM2 Degrader-2 is an MDM2 PROTAC degrader. PROTAC MDM2 Degrader-2 can induce the self-ubiquitination and degradation of MDM2, thereby upregulating the level of p53 protein. PROTAC MDM2 Degrader-2 has anti-tumor activity and can be used in the study of cancer . (Blue: MDM2 ligand (HY-128836); Black: linker (HY-128833))
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- HY-128839
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PROTACs
Estrogen Receptor/ERR
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Cancer
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PROTAC ERRα Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader .
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- HY-161615
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Apoptosis
PROTACs
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Cancer
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PROTAC ATR degrader-2 (Compound 8i) is a PROTAC degrader for ATR, through of . PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 of 22.9 and 34.5 nM. APROTAC ATR degrader-2 induces apoptosis, inhibits proliferations of AML cells. PROTAC ATR degrader-2 exhibits good pharmacokinetics charachers and antitumor efficacy against AML in mouse model. (Pink: ATR ligand (HY-161616); Blue:E3 ligase ligand Lenalidomide (HY-A0003); Black: linker)
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- HY-153023
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PROTACs
STAT
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Cancer
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PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC50 of 3.54 μM in Molm-16 Cell. PROTAC STAT3 degrader-2 has the potential for cancer research . PROTAC STAT3 degrader-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-145395
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PROTACs
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Cancer
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PROTAC BRD9 Degrader-2 is a BRD9 bifunctional degrader for researching cancer.
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- HY-157164
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PROTACs
Histone Methyltransferase
Apoptosis
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Cancer
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PROTAC EZH2 Degrader-2 is a PROTAC EZH2 inhibitor. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner. PROTAC EZH2 Degrader-2 induces apoptosis and reduces mitochondrial membrane potential in SU-DHL-6 cells. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity. (Pink: EZH2 ligand (HY-15335), Blue: MDM2 Ligand (HY-147230), Black: Linker (HY-175707), EZH2 ligand-linker conjugate (HY-175706)) .
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- HY-164365
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PROTACs
Ras
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Cancer
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PROTAC K-Ras degrader-2 (compound 48) is a pan-KRAS-mutant PROTAC degrader with an IC50 of ≤200 nM for KRAS G12V/RAF1. PROTAC K-Ras degrader-2 degrades SW620 KRAS G12D with a DC50 of ≤200 nM. PROTAC K-Ras degrader-2 inhibits cell growth of SW620 3D cell with an IC50 of ≤20 nM. (Pink: KRAS inhibitor-30 (HY-164366)) .
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- HY-158036
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PROTACs
STING
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Others
Inflammation/Immunology
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PROTAC STING degrader-2 is a protein Degrader that targets Stimulator of interferon genes (STING) (DC50=0.53 μM). PROTAC STING Degrader-2 is combined with STING protein and E3 ubiquitin ligase in a covalent manner to induce the degradation of STING protein. PROTAC STING Degrader-2 can be used to investigate the role of STING in autoinflammation and autoimmune diseases (PINK: STING binder (HY-145009); Blue: VHL ligand (HY-164043); Black: linker) .
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- HY-156153
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Histone Methyltransferase
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Cancer
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PROTAC CARM1 degrader-2 (compound 3e) is a degrader (DC50=8.8 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-2 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-2 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .
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- HY-163938A
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PROTACs
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Cancer
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PROTAC erf3a Degrader-2 (Compound C59) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-2 inhibits protein expression of SRD5A3 and GSPT1(eRF3a). PROTAC erf3a Degrader-2 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-2 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: E3 ligase ligand (HY-W763812)) .
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- HY-130615
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PROTACs
Histone Methyltransferase
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Cancer
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PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit .
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- HY-149948
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer .
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- HY-112557
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PROTACs
IKK
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Cancer
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PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM) .
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- HY-137488
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PROTACs
Raf
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Cancer
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PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth .
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- HY-174444
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PROTACs
HDAC
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Cancer
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PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC50s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs. ( Pink: HDAC ligand : (HY-174471), Blue: E3 ligase CRBN Ligand (HY-131717), E3 ligase ligand-linker conjugate (HY-174473)) .
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- HY-174136
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STING
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Inflammation/Immunology
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STING Degrader-2 (Compound SI-43) is a STING inhibitor and mutant-specific degrader. STING Degrader-2 can effectively inhibit cGAMP-induced STING activation and significantly reduce the release of IFN-β and CXCL-10. It inhibits the activity of STING by binding to two pockets of the STING dimer and induces proteasome-independent degradation of mutants STING S154 and STING M155 (DC50 values are 0.31 and 0.76 μM, respectively). STING Degrader-2 can be used to study STING-related autoimmune diseases .
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- HY-153821
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Ras
PROTACs
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Cancer
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PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS .
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- HY-169072
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PROTACs
Mixed Lineage Kinase
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Cancer
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PROTAC MLKL Degrader-2 (compound MP-1) is a PROTAC targeting MLKL (Mixed Lineage Kinase). PROTAC MLKL Degrader-2 is composed of PROTAC target protein ligand PROTAC MLKL Degrader-2 (HY-169072) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part) and PROTAC Linker N-Methylpiperazine (HY-78871) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-N-methylpiperazine (HY-169074) [1] .
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- HY-132194
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Estrogen Receptor/ERR
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Cancer
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ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER + breast cancer research .
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- HY-163639
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Molecular Glues
Epigenetic Reader Domain
E1/E2/E3 Enzyme
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Cancer
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BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue BRD4degrader that induces a ternary complex formation between BRD4 and RNF126. BRD4 degrader-2 targets RNF126 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells .
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- HY-153425
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PROTACs
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Cancer
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PROTAC SMARCA2 degrader-2 is a potent and selective SMARCA2/4 PROTAC degrader with an IC50 of <0.1 μΜ in HeLa HiBiT assay. PROTAC SMARCA2 degrader-2 is extracted from patent WO2023287787A1 and has the potential for SMARCA4-related or deficient cancer research .
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- HY-143905
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PROTACs
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Cancer
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PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
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- HY-111846
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PROTACs
Estrogen Receptor/ERR
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Cancer
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PROTAC ERα Degrader-2 (Compound 11) is a ERα PROTAC degrader. PROTAC ERα Degrader-2 significantly down-regulates the level of ERα in MCF-7 cells.(Pink: AR ligand (HY-43962), Blue: IAP Ligand (HY-177389), Black: Linker (HY-128833)) .
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- HY-111841
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SNIPERs
PROTACs
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Cancer
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PROTAC CRABP-II Degrader-2 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand .
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- HY-111866
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PROTACs
RIP kinase
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Metabolic Disease
Cancer
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PROTAC RIPK degraders -2 is a non-peptide PROTAC based on von Hippel-Lindau and targets serine-threonine kinase RIPK2, which is highly selective to the degradation of RIPK2. PROTAC RIPK degrader-2 acts as an activator to increase cell death and activate ion channels in cancer cells. PROTAC RIPK degrader-2 also can inhibit protein interactions, such as receptors and ligands, involved in a variety of diseases, such as cancer and diabetes .
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- HY-153938
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- HY-161750
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PROTACs
Anaplastic lymphoma kinase (ALK)
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Cancer
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PROTAC ALK degrader-2 (B1-PEG) is an ALK degrader based on PROTACs, with the DC50 of 45 nM in H3122 EML4-ALK DC50 (GSH+). PROTAC ALK degrader-2, through PEGylation, is engineered to self-organize into micelles in water and releases its active form in response to the tumor-specific high GSH environment .
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- HY-162972
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PROTACs
PD-1/PD-L1
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Cancer
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PROTAC PD-L1 degrader-2 (Compound 9i) is a PROTAC degrader for PD-L1, that inhibits PD-L1 with an IC50 of 197.4 nM and exhibits an affinity with PD-L1 with a Kd of 301 nM. PROTAC PD-L1 degrader-2 promotes the internalization of PD-L1 on the cell membrane, and induces PD-L1 degradation via the synergistic effect of the proteasome and lysosomal pathways. PROTAC PD-L1 degrader-2 can activate the immune system, and exhibits antitumor efficacy in MC38 C57BL/6 mouse model .
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- HY-156795
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CDK
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Cancer
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PROTAC CDK9/CycT1 Degrader-2 is a inhibitor of CDK9, with the IC50 of 45 nM .
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- HY-153938A
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- HY-149679
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PROTACs
Bacterial
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Cancer
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PROTAC eDHFR Degrader-2 (compound 7b) is a potent degrader targeting Escherichia coli dihydrofolate reductase (eDHFR), enabling robust degradation of eDHFR-tagged proteins .
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- HY-164306
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PROTACs
PARP
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Cancer
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PROTAC PARP1 degrader-2 (Compound 72) is a PROTAC degrader for PARP with a DC50<10 nM in MDA-MB-231 cell. PROTAC PARP1 degrader-2 inhibits the cell viability of MDA-MB-436 with an IC50 <100 nM. (Blue: ligand for target protein (HY-160937); Pink: ligand for E3 ligase (HY-W998262))
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- HY-174368
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Pro-BA
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PROTACs
Apoptosis
Anaplastic lymphoma kinase (ALK)
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Cancer
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PROTAC EML4-ALK Degrader-2 (Pro-BA) is a selective and orally active linker-free EML4-ALK PROTAC degrader with the DC50 of 74 nM in H1322 cells (T1/2 = 8 h). PROTAC EML4-ALK Degrader-2 relies on GID4 and proteasome pathways to promote ubiquitination of target proteins, leading to cell apoptosis. PROTAC EML4-ALK Degrader-2 can be used for research on cancer. (Pink: EML4-ALK Ligand (HY-40114); Blue: GID4 Ligand (HY-150908))
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- HY-178803
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PROTACs
BCL6
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Cancer
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PROTAC BCL6 Degrader-2 (Compound A19) is an orally active, selective BCL6 PROTAC degrader (DC50s: 34 pM in OCI-LY1 cells and 0.45 nM in HEK293T cells). PROTAC BCL6 Degrader-2 promotes the ubiquitination and degradation of BCL6. PROTAC BCL6 Degrader-2 exhibits anticancer activity against BCL6-dependent diffuse large B-cell lymphoma (Pink: BCL6 ligand (HY-178804); Blue: E3 ligase ligand (HY-W087383); E3 ligase ligand + linker (HY-W998306)) .
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- HY-174469
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PROTACs
P-glycoprotein
Apoptosis
Reactive Oxygen Species (ROS)
Akt
Bcl-2 Family
Na+/K+ ATPase
PI3K
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Cancer
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PROTAC PI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. PROTAC PI3K/110β degrader-2 can significantly degrade 110β protein and inhibit the expression of P-glycoprotein. PROTAC PI3K/110β degrader-2 can increase the level of reactive oxygen species (ROS). PROTAC PI3K/110β degrader-2 exerts anti-tumor effects by activating the endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. PROTAC PI3K/110β degrader-2 can be used for research on cancer. (Pink: PI3K/110β Ligand (HY-75124); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W002042)) .
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- HY-163813
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- HY-150908
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Ligands for E3 Ligase
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Cancer
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Brigatinib A is an GID4 ligand. Brigatinib A can be used for synthesizing PROTAC BCR-ABL Degrader-2 (HY-174368) .
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- HY-168176
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PROTACs
HDAC
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Cancer
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HDAC8 ligand 1 is a PROTAC target protein-ligand of PROTAC HDAC8 Degrader-2 (HY-168174) .
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- HY-43538
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PROTAC Linkers
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Cancer
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5-Bromopentanoyl chloride is a PROTAC linker in PROTAC ATR degrader-2 (HY-161615), and can be used for synthesis of PROTACs .
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- HY-157805
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PROTACs
SARS-CoV
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Infection
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PROTAC SARS-CoV-2 Mpro degrader-2 (Compound 6) is a potent PROTAC degrader of SARS-CoV-2 M pro. PROTAC SARS-CoV-2 Mpro degrader-2 has broad-spectrum antiviral activity against CoVs, including SARS-CoV-2 (EC50 = 10.8 μM), HCoV-OC43 (EC50 = 1.6 μM) and HCoV-229E (EC50 = 6.5 μM). PROTAC SARS-CoV-2 Mpro degrader-2 exhibits potent activity against SARS-CoV-2 in Calu-3 cells, with an EC50 of 0.89 μM .
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- HY-139309
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Bcl-2 Family
PROTACs
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Cancer
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PROTAC Bcl-xL degrader-2 is a potent Bcl-xL (Bcl-2 family member) degrader based on von Hippel-Lindau ligand, with an IC50 of 0.6 nM.
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- HY-161616
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ATM/ATR
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Cancer
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ATR-IN-30 is a selective ATR ligand, and can be used for synthesis of ATR PROTACs, such as PROTAC ATR degrader-2 (HY-161615) .
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- HY-174471
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- HY-174225
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- HY-177389
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- HY-W007700
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PROTAC Linkers
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Cancer
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8-Bromooctanoic acid is a PROTAC linker, and can be used for synthesis of PROTAC CYP1B1 degrader-2 (HY-158429) .
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- HY-133136
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- HY-176388
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- HY-174473
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- HY-169363
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PD-1/PD-L1
Autophagy
AUTACs
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Cancer
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PD-L1 degrader-2 (Compound B3) is an orally active AUTAC degrader, that degrades PD-L1 through autophagy-lysosome pathway with a DC50 of 0.5 μM. PD-L1 degrader-2 exhibits inhibitory activity against PD-1/PD-L1 interaction with an IC50 of 22.8 nM. PD-L1 degrader-2 upregulates the expressions of Atg9b, Lamp1 and Mitf, and activates the autophagy lysosome system. PD-L1 degrader- exhibits antitumor efficacy in CT26 mouse model . (Pink: autophagy-lysosome activator (HY-159894); Black: linker (HY-W015088); Blue: PD-L1 ligand (HY-169365))
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- HY-176804
-
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Ligands for E3 Ligase
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Cancer
|
|
(R,S,R)-AHPC-Me-Ac is an E3 ligase ligand used in the synthesis of the PROTAC SHP2 Protein degrader-2 (HY-145703) .
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-
- HY-174443
-
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PROTACs
Epoxide Hydrolase
|
Neurological Disease
Inflammation/Immunology
|
|
PROTAC sEH degrader-2 is a PROTAC targeting degradation agent for soluble epoxide hydrolase (sEH) with pIC50 values of the catalytic domain of 8.37 (human sEH-H) and 7.12 (mouce sEH-H). PROTAC sEH degrader-2 can be used for the research related to inflammation and neuroinflammation, such as Alzheimer's disease . (Structure Note: Pink: sEH-H ligand (HY-174225); Blue: CRBN Ligand (HY-103597); Black: linker; E3 + linker (HY-141011))
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-
- HY-120217A
-
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Ligands for E3 Ligase
|
Cancer
|
|
(S,S,S)-VH032 is the ligand for E3 Ligase (VHL) that can be used for synthesis of PROTAC SGK3 degrader-2 (HY-176823) .
|
-
- HY-168248
-
-
- HY-130850
-
-
- HY-163865
-
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PROTACs
|
Cancer
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|
SMARCA2 degrader-2 (compound I-322) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
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-
- HY-176823
-
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PROTACs
SGK
|
Cancer
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|
PROTAC SGK3 degrader-2 is the cis epimer of PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (HY-125878), with a cis hydroxyl group in its VH032 moiety, which is incapable of binding to the VHL E3 ligase. PROTAC SGK3 degrader-2 exhibits inhibitory activity against SGK3, SGK1, and S6K1 with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but shows no SGK3 degradation efficiency. PROTAC SGK3 degrader-2 can be used as a control compound to study the specific effects of SGK3-PROTAC1-mediated SGK3 degradation. (Pink: SGK3 ligand (HY-167701), Blue: VHL Ligand (HY-120217A), Black: Linker (HY-130618), SGK3 ligand-linker conjugate (HY-176824)) .
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-
- HY-176864
-
-
- HY-114228
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PROTACs
Epigenetic Reader Domain
|
Cancer
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|
PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
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-
- HY-W998262
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
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|
Pomalidomide 5-piperidylamine is the conjugate of an E3 ligase ligand and a linker. Pomalidomide 5-piperidylamine can be used for synthesis of PROTAC PARP1 degrader-2 (HY-164306) .
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-
- HY-176334
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-
- HY-164043
-
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Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC(Me)-amido-C2-acid is an VHL (E3 ligase) ligand, and can be used for synthesis of PROTACs, such as PROTAC STING Degrader-2 (HY-158036) .
|
-
- HY-162546
-
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|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
3-hydroxypropanoic acid-pip-hydroquinone-dihydrouracil is a conjugate of E3 ligase ligand and linker that serve as a key intermediate for the synthesis of complete PROTAC HPK1 Degrader-2 (HY-162544) .
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-
- HY-168249
-
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PROTAC Linkers
|
Cancer
|
|
trans-4-(2-Chloropyrimidin-5-yl)cyclohexanecarboxylic acid is a PROTAC Linker that can be used to synthesize PROTAC BRM/BRG1 degrader-2 (HY-168247) .
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-
- HY-161749
-
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PROTACs
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
PROTAC ALK degrader-1 (compound B1) is an ALK degrader based on PROTACs, with the DC50 of 26 nM in H3122 EML4-ALK. PROTAC ALK degrader-1 can be used to synthesis PROTAC ALK degrader-2 (HY-161750) with superior bioavailability .
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-
- HY-171334
-
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PROTACs
PIN1
|
Cancer
|
|
PROTAC PIN1 degrader-2 (1) is a PROTAC-based PIN1 degrader (Pink: PIN1 ligand HY-171442, Blue: cereblon ligand Thalidomide (HY-14658), Black: linker HY-W014883). PROTAC PIN1 degrader-2 (1) possesses anti-cancer activity, with IC50 values of 2248 nM (MV-4-11 cells), 3984 nM (MOLM-13), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60) and 3925 nM (HL-60) respectively .
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-
- HY-158429
-
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|
PROTACs
Cytochrome P450
|
Cancer
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|
PROTAC CYP1B1 degrader-2 (compound PV2) is a von Hippel-Landau (VHL) E3 ligase-based CYP1B1 degrader with the DC50 of 1.0 nM at 24 h in A549/Taxol cells. PROTAC CYP1B1 degrader-2 inhibits growth, migration, and invasion of A549/Taxol cell(Sturcture Note:(Blue: VHL ligand (HY-112078), Black: linker (HY-W007700), Pink: CYP1B1 ligand (HY-159006) .
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-
- HY-158431
-
-
- HY-162841
-
-
- HY-W761300
-
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|
Ligands for E3 Ligase
|
Others
|
|
1-(4-Pip-Ph)-DHP-dione is an E3 ligase ligand. 1-(4-Pip-Ph)-DHP-dione can be used for synthesis of PROTAC HPK1 Degrader-2 (HY-162544) .
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-
- HY-158430
-
-
- HY-168250
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
trans-(S,R,S)-AHPC-Me-Amide-cyclohexane-pyrimidine-Cl is a E3 ligase ligand-linker conjugate, and can be used for synthesis of PROTACs, such as PROTAC BRM/BRG1 degrader-2 (HY-168247) .
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-
- HY-169073
-
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Ligands for Target Protein for PROTAC
|
Others
|
|
TC13172-NH-COOH is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). TC13172-NH-COOH can be used for synthesis PROTAC MLKL Degrader-2 (HY-169072) .
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-
- HY-162840
-
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-azetidin-3-one is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-azetidin-3-one can be used to synthesize PROTAC PD-L1 degrader-2 (HY-162816) .
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-
- HY-162842
-
-
- HY-163961A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-cyclohexane-NH-Ph-NH2 is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-NH-cyclohexane-NH-Ph-NH2 can be used to synthesize PROTAC erf3a Degrader-2 (HY-163938A) .
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-
- HY-169074
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|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-N-methylpiperazine is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-N-methylpiperazine can be used to synthesize PROTAC MLKL Degrader-2 (HY-169072) to exhibit antinecroptotic activity on human cell lines and effectively degrade MLKL in the HT-29 xenograft mouse model .
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-
- HY-112811
-
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PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-2 (compound 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC .
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-
- HY-176477
-
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Epigenetic Reader Domain
FKBP
|
Cancer
|
|
BRD4/FKBP12 degrader-2 (a1dj) is a BRD4/FKBP12 degrader and shows anticancer activity (BRD4 ligand: HY-78695, FKBP12 ligand: HY-176502, linker: HY-140212) .
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-
- HY-128528
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|
PROTAC-Linker Conjugates for PAC
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ER Degrader-2 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
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-
- HY-176335
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-
- HY-170335
-
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|
PROTACs
c-Met/HGFR
|
Others
|
|
PROTAC c-Met degrader-2 (PROTAC2) is a PROTAC-based c-Met degrader, with a DC50 of 50 nM (Pink: Foretinib (HY-10338); Black: linker (HY-45124); Blue: CRBN ligand Thalidomide-4-O-C2-NH2 (HY-136162A)) .
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-
- HY-178804
-
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|
Ligands for Target Protein for PROTAC
BCL6
|
Cancer
|
|
BCL6 ligand-5 (Compound 37) is a BCL6 ligand. BCL6 ligand-5 can be used as a ligand for target protein for PROTAC to develop and design degraders for PROTAC BCL6, such as PROTAC BCL6 Degrader-2 (HY-178803). BCL6 ligand-5 can also be used in tumor research .
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-
- HY-161675
-
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|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-5-bromopentanamide is an E3 ligase ligand-linker conjugate in PROTAC ATR degrader-2 (HY-161615), and consists of a CRBN ligand Lenalidomide (HY-A0003) and a linker 5-Bromopentanoyl chloride (HY-43538). Lenalidomide-5-bromopentanamidecan be used for synthesis of PROTACs .
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-
- HY-159006
-
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Cytochrome P450
|
Cancer
|
|
CYP1B1 ligand 3 (Compound A1) is a selective inhibitor for cytochrome P450 enzyme CYP1B1 with an IC50 of 11.9 nM. CYP1B1 ligand 3 can be utilized for the synthesis of PROTAC CYP1B1 degrader-2 (HY-158429) .
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-
- HY-162545
-
|
|
MAP4K
Ligands for Target Protein for PROTAC
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Cancer
|
|
HPK1-IN-47 is a HPK1 ligand. HPK1-IN-47 can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-2 (HY-162544). HPK1-IN-47 can be used for research of HPK1-mediated diseases including cancer .
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-
- HY-168247
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRM/BRG1 degrader-2 (Example.004) is a PROTAC BRM/BRG1 degrader (DC50: < 10 nM in A549 cell; IC50: 15 nM for A549). Blue: E3 ligase ligand (HY-112078), Black: linker (HY-168249), Pink: BRM/BRG1 inhibitor (HY-168248) .
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-
- HY-130815A
-
-
- HY-130815
-
-
- HY-W1120221
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
Lenalidomide-C3-NH2 is an E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based CRBN ligand (HY-43722) and linker. Lenalidomide-C3-NH2 can be used for synthesis of PROTAC BET degrader-2 (HY-114228) .
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-
- HY-168175
-
|
|
PROTACs
HDAC
|
Cancer
|
|
PROTAC HDAC8 Degrader-2 (compound 32a) is a degrader of HDAC8 with a DC50 of 8.9 nM and HDAC6 with a DC50 of 14.3 nM. PROTAC HDAC8 Degrader-2 is composed of PROTAC target protein ligand HDAC8 ligand 1 (HY-168176) (red part), E3 ligase ligand Thalidomide-4-OH (HY-103596) (blue part) and PROTAC Linker 1,5-Diaminopentane (HY-W540541) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C5-NH2 (HY-134986) .
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-
- HY-150251
-
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STAT3 degrader-2
|
PROTACs
STAT
|
Cancer
|
|
SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a Ki of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506) .
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-
- HY-133139
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Lenalidomide-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker.?Lenalidomide-PEG1-azide?can be used to design a PROTAC BRD4 Degrader-2 (HY-133136) . Lenalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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-
- HY-160533
-
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Molecular Glues
IKZF Family
|
Cancer
|
|
IKZF1-degrader-2 (Compound 3) is an IKZF1 molecular glues degrader. IKZF1-degrader-2 has anticancer activity and low toxicity .
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-
- HY-W1128213
-
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|
Molecular Glues
IKZF Family
|
Inflammation/Immunology
Cancer
|
|
IKZF2-degrader 2 is a selective and orally active IKZF2 molecular glue degrader with DC50 values of 0.5 nM and 1.8 nM in HiBit and FACS. The IKZF2-degrader 2 mediates the ubiquitination and degradation of target proteins by recruiting the CRL4-CRBN E3 ubiquitin ligase. IKZF2-degrader 2 displays moderate degradation against SALL4 with a DC50 of 9 nM but does not induce any significant degradation towards IKZF1, IKZF3, CK1α and GSPT1. IKZF2-degrader 2 can be used for the study of cancer immunology .
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-
- HY-144627
-
|
|
PROTACs
TAM Receptor
|
Cancer
|
|
PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 μM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis .
|
-
- HY-144304
-
|
|
PROTACs
EGFR
|
Cancer
|
|
PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC .
|
-
- HY-172882
-
|
|
Molecular Glues
IKZF Family
|
Cancer
|
|
IKZF2-degrader 1 (Compound 31) is a IKZF2 molecular glue degrader, with an DC50 of 0.5 nM. IKZF2-degrader 1 has minimal CK1α degradation activity relatively (DC50: 210 nM). IKZF2-degrader 1 can be used for research of IKZF2-dependent cancers .
|
-
- HY-153322
-
|
|
PROTACs
Itk
|
Cancer
|
|
ITK degrader 2 (compound 30) is an orally active, PROTAC-based ITK-targeted degrader (DC50<10 nM). ITK degrader 2 exhibits Cmax and Tmax in mice (po; 90 mg/kg) of 0.87 μM and 2 h, respectively. At this dose, ITK degrader 2 degrades ITK by 20% (6 h) in mice .
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-
- HY-163818
-
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|
Histone Methyltransferase
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Others
|
|
WIZ degrader 2 (Compound 142) is a degrader for widely interspaced zinc finger motifs with an AC50 of 0.011 μM. WIZ degrader 2 induces the expression of fetal hemoglobin (HbF) with an EC50 of 0.038 μM. WIZ degrader 2 can be used in research about inherited blood disorders .
|
-
- HY-171139
-
|
|
PROTACs
HDAC
|
Cancer
|
|
PROTAC HDAC6 degrader 2 (Compound 1) is a HDAC6 PROTAC degrader, with IC50 of 0.643 μM. PROTAC HDAC6 degrader 2 promotes ubiquitination and degradation of HDAC6. PROTAC HDAC6 degrader 2 can be used for the research of haematological and solid cancers (Pink: HDAC6 ligand (HY-171141); Blue: E3 ligase CRBN ligand (HY-10984)) .
|
-
- HY-163759
-
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|
Molecular Glues
HuR
|
Cancer
|
|
HuR degrader 2 (Compound 3) is a molecule glue, which targets RNA-binding protein Hu antigen R (HuR) and degrades 30% HuR at 0.1 μM. HuR degrader 2 inhibits the proliferation of cancer cell Colo-205, with IC50≤200 nM. HuR degrader 2 exhibits a high affinity with cereblon, with an HTRF ratio < 0.02 .
|
-
- HY-175527
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
ALK degrader 2 is an orally active ALK degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)) .
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-
- HY-159453
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2/4-degrader-2 (compound I-431) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-159662
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
HSD17B13 degrader 2 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). HSD17B13 degrader 2 can be used for synthesis PTOTAC HSD17B13 degrader 1 (HY-159651) .
|
-
- HY-142926
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 2 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 2 has the potential for the research of cancer diseases (extracted from patent CN112830919A, compound 1) .
|
-
- HY-146369
-
|
|
PROTACs
VEGFR
|
Cancer
|
|
PROTAC VEGFR-2 degrader-2(PROTAC-4), a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100μM) .
|
-
- HY-176824
-
-
- HY-163709
-
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|
PROTACs
FAK
|
Cancer
|
|
PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC50 of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC50s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))
|
-
- HY-159594
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Dimethylformamide-(S,R,S)-AHPC-CO-cyclohexane-pyrimidine-diazabicyclo is an E3 Ligase Ligand-Linker Conjugate. Dimethylformamide-(S,R,S)-AHPC-CO-cyclohexane-pyrimidine-diazabicyclo can be used to synthesize PROTAC SMARCA2/4-degrader-2 (HY-159453) .
|
-
- HY-159454
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2/4-degrader-3 (compound I-433) is a PROTAC SMARCA2/4-degrader based on VH032-NH2, with a degradation potency (DC50) <100 nM in MV4-11 cells .
|
-
- HY-169135
-
|
|
PROTACs
Proteasome
|
Cancer
|
|
PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader for 20S proteasome subunit β5, with a DC50 of 0.16 μM. PROTAC 20S proteasome subunit β5 degrader 2 inhibits the proliferation of cancer cell FaDu with IC50 of 0.23 μM. PROTAC 20S proteasome subunit β5 degrader 2 exhibits antitumor efficacy in mice models . (Pink: Ligand for target protein (HY-10227); Blue: Ligand for E3 ligase (HY-103596); Black: Linker (HY-Y1760))
|
-
- HY-178516
-
|
|
CDK
PROTACs
|
Cancer
|
|
PROTAC CDK4/6/9 degrader 2 (Compound P4) is a CDK4/6/9 PROTAC prodrug with oral activity and low toxicity. PROTAC CDK4/6/9 degrader 2 can significantly inhibit tumor growth and suppress tumor lung metastasis. PROTAC CDK4/6/9 degrader 2 can be used in the research of cancer such as breast cancer. (Pink: CDK4/6/9 Ligand (HY-168440); Blue: CRBN Ligand (HY-178517); Black: Linker (HY-178512))
|
-
- HY-W687952
-
|
|
PROTAC Linkers
|
Others
|
|
Piperidine-C-piperidine-Boc is a PROTAC linker. Piperidine-C-piperidine-Boc is the linker of CDK2 degrader 2 (HY-163815) .
|
-
- HY-45512
-
-
- HY-176043
-
|
|
ATTECs
PCSK9
|
Cancer
|
|
PCSK9 autophagic degrader 2 (W6) is a PCSK9 targeted autophagosome, with an DC50 of 20.6 nM. PCSK9 autophagic degrader 2 (W6) demonstrates comparable antiatherosclerosis effect and exhibits a KD of 2.5 μM for LC3B (Pink: PCSK9 ligand HY-176044; Blue: LC3B ligand HY-176045; Black: linker HY-141373) .
|
-
- HY-176044
-
-
- HY-171141
-
-
- HY-163815
-
|
|
PROTACs
CDK
|
Cancer
|
|
CDK2 degrader 2 (Compound I-10) is a PROTAC degrader for CDK2 that degrades CDK2 in MKN1 cell with a DC50 <100 nM . (Pink: ligand for target protein (HY-176124); Black: linker (HY-W687952); Blue: ligand for E3 ligase CRBN (HY-45512))
|
-
- HY-176045
-
|
|
Ligands for E3 Ligase
|
Cardiovascular Disease
Cancer
|
|
LC3B ligand 2 is a ligand for E3 ubiquitin ligase. LC3B ligand 2 can be connected to the ligand for protein by a linker to form PROTAC PCSK9 autophagic degrader 2 (HY-176043). PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
|
-
- HY-176124
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
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CDK2 ligand-2 is a PROTAC target protein ligand (Ligands for Target Protein for PROTAC). CDK2 ligand-2 combined with E3 Ligase Ligand-linker Conjugate 184 (HY-176125) can be used to synthesize PROTAC degrader (CDK2 degrader 2 (HY-163815)) .
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- HY-168543
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PROTACs
Aurora Kinase
Mps1
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Cancer
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PROTAC MPS1 degrader 2 (Compound 15) is a potent degrader of monopolar spindle 1 (Mps1,TTK),AURKA and AURKB,with DC50s of 42.0,2.1 and 154.0 nM,respectively. PROTAC MPS1 degrader 1 can be used for the research of acute myeloid leukemia. (Pink: ligand for target protein (HY-168545); Black: linker (HY-N0420); Blue: ligand for E3 ligase (HY-10984) .
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- HY-W017389S1
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Endogenous Metabolite
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Neurological Disease
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Xanthine- 15N2 is a 15N-labeled Xanthine (HY-W017389) . Xanthine, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine also acts as an intermediate product on the pathway of purine degradation .
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- HY-176046
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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E3 Ligase Ligand-linker Conjugate 183 is an E3 ligase ligand-linker conjugate of PCSK9 autophagic degrader 2 (HY-176043). E3 Ligase Ligand-linker Conjugate 183 consists of LC3B ligand 2 (HY-176045) and the corresponding linker (HY-141373) .
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- HY-159651
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PROTACs
17β-HSD
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Cancer
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PTOTAC HSD17B13 degrader 1 (compound 1) is a PROTAC targeting 17β-HSD 13 (HSD17B13). PTOTAC HSD17B13 degrader 1 is composed of PROTAC target protein ligand HSD17B13 degrader 2 (HY-159662) (red part), PROTAC Linker tert-Butyl 5-bromoisoindoline-2-carboxylate (HY-W003696) (black part) and E3 ubiquitin ligase ligand E3 ligase Ligand 31 (HY-159660) (blue part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 114 (HY-159661) [1] .
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- HY-176125
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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E3 Ligase Ligand-linker Conjugate 184 is a E3 Ligase Ligand-Linker Conjugates, consisting of CDK2 ligand-2 (HY-176124) and the corresponding Linker. E3 Ligase Ligand-linker Conjugate 184 can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete CDK2 degrader 2 (HY-163815) .
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- HY-178517
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E1/E2/E3 Enzyme
Ligands for E3 Ligase
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Cancer
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Thalidomide-C1-O-CO-C2 is a ligand for E3 ubiquitin ligase. Thalidomide-C1-O-CO-C2 can be connected to Aurora-A ligand 1 (HY-168440) by a linker (HY-178512) to form PROTAC CDK4/6/9 degrader 2 (HY-178516) .
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- HY-178518
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E3 Ligase Ligand-Linker Conjugates
E1/E2/E3 Enzyme
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Cancer
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Thalidomide-OCH2-amide-PEG2-C2-Boc is an E3 ligase ligand-linker conjugate containing a cereblon (CRBN) ligand for E3 ubiquitin ligase and a linker. Thalidomide-OCH2-amide-PEG2-C2-Boc can be used to synthesize PROTAC CDK4/6/9 degrader 2 (HY-178516) .
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Product Name |
Chemical Structure |
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- HY-W017389S1
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Xanthine- 15N2 is a 15N-labeled Xanthine (HY-W017389) . Xanthine, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine also acts as an intermediate product on the pathway of purine degradation .
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Product Name |
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Classification |
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- HY-133139
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PROTAC Synthesis
Azide
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Lenalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Lenalidomide-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker.?Lenalidomide-PEG1-azide?can be used to design a PROTAC BRD4 Degrader-2 (HY-133136) . Lenalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-143905
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PROTAC Synthesis
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PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
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- HY-174225
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Alkynes
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sEH-H ligand 1 is a PROTAC target protein ligand that can be used to synthesize PROTAC sEH degrader-2 (HY-174443) .
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- HY-174473
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Alkynes
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Thalidomide-NH-alkynes is a synthesized E3 ligase ligand-linker conjugate that can be used for synthesis of PROTAC HDAC degrader-2 (HY-174444) .
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- HY-150251
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STAT3 degrader-2
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PROTAC Synthesis
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SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a Ki of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506) .
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- HY-159453
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Azide
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SMARCA2/4-degrader-2 (compound I-431) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
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- HY-159454
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Azide
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SMARCA2/4-degrader-3 (compound I-433) is a PROTAC SMARCA2/4-degrader based on VH032-NH2, with a degradation potency (DC50) <100 nM in MV4-11 cells .
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