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-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-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-161615
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PROTACs
ATM/ATR
Apoptosis
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Inflammation/Immunology
Cancer
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PROTAC ATR degrader-2 is a selective ATR PROTAC degrader. PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 values of 22.9 nM and 34.5 nM, respectively. PROTAC ATR degrader-2 has an IC50 of 29.6 nM against ATR, and its IC50 values against ATM and PI3K are both greater than 2000 nM. PROTAC ATR degrader-2 induces apoptosis, DNA damage, and upregulates p53 expression. PROTAC ATR degrader-2 inhibits cancer cell proliferation through the kinase-independent function of ATR protein. PROTAC ATR degrader-2 is applicable to research related to acute myeloid leukemia .
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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-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-168624
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Molecular Glues
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Inflammation/Immunology
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VAV1 degrader-2 is a molecular glue degrader based on targeting Vav guanine nucleotide exchange factor 1 (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-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-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-133136
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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-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 .
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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-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-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-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-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-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-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-158036
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PROTACs
STING
IKK
IFNAR
CXCR
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Inflammation/Immunology
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PROTAC STING Degrader-2 is a STING PROTAC degrader with a DC50 of 0.53 μM. PROTAC STING Degrader-2 reduces the phosphorylation levels of TBK1 and IRF3. PROTAC STING Degrader-2 decreases the mRNA expression levels of IFN-β, CXCL10 and TNF-α, and blocks luciferase secretion. PROTAC STING Degrader-2 can be used in the research of autoimmune diseases .
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- HY-174136
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STING
IFNAR
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Inflammation/Immunology
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STING Degrader-2 is an orally active STING degrader that promotes proteasome-independent degradation of STING. STING Degrader-2 inhibits cGAMP-induced STING activation, suppresses STING oligomerization, and inhibits phosphorylation of STING and interferon regulatory factor 3 (IRF3). STING Degrader-2 reduces serum IFN-β and CXCL-10 levels in a cGAMP-induced autoimmune disease mouse model. STING Degrader-2 can be used for the research of autoimmune diseases .
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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-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-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-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-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-153938
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PROTACs
Phosphatase
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Metabolic Disease
Cancer
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PROTAC PTPN2 degrader-2 is a potent PTPN2 PROTAC degrader with a DC50 of <50 nM. PROTAC PTPN2 degrader-2 is potential for studying cancer or metabolic diseases, such as colon cancer .
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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 KRAS G12V PROTAC degrader with an IC50 of 20-200 nM for KRAS G12V/RAF1. PROTAC K-Ras degrader-2 degrades SW620 KRAS G12V with a DC50 of 1-10 nM. PROTAC K-Ras degrader-2 inhibits cell growth of SW620 3D cell with an IC50 of ≤10 nM. PROTAC K-Ras degrader-2 can be used for the study of colorectal cancer (CRC) .
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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-179233
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PROTACs
STAT
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Cancer
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PROTAC STAT6 degrader-2 is a highly efficient PROTAC degrader targeting STAT6. PROTAC STAT6 degrader-2 has a DC50 value of 1-10 nM for STAT6 in human PBMC cells and a DC50 value of less than 100 nM for STAT6 in HEK293-HIBiT-STAT6 cells. PROTAC STAT6 degrader-2 can be used for STAT6-mediated diseases .
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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-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-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-120217A
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Ligands for E3 Ligase
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Cancer
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(S,S,S)-VH032 is the ligand for E3 Ligase (VHL) that can be used for synthesis of PROTAC SGK3 degrader-2 (HY-176823) .
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- HY-114228
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PROTACs
Epigenetic Reader Domain
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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-176864
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- HY-176334
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- HY-179388
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PROTACs
Sirtuin
Apoptosis
Akt
mTOR
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Cancer
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PROTAC Sirt2 Degrader-2 is a highly efficient and selective PROTAC degrader targeting SIRT2. PROTAC Sirt2 Degrader-2 demonstrates the most potent anti-proliferative activity both in vitro and in vivo. PROTAC Sirt2 Degrader-2 leads to a marked increase in H4K16Ac levels. PROTAC Sirt2 Degrader-2 significantly suppresses clonogenic formation and migration, induces cell cycle arrest, and promotes apoptosis. PROTAC Sirt2 Degrader-2 inhibits the AKT/mTOR signaling pathway by indirectly degrading SIRT2 and blocking downstream protein phosphorylation, thereby disrupting the signaling cascade and suppressing tumor development. PROTAC Sirt2 Degrader-2 can be used for the study of ovarian cancer .
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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 (Compound C1) 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-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-179562
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Btk
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Cancer
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BTK degrader-2 (Example 2) is a BTK dual-functional degrading agent, which causes the degradation of BTK through the ubiquitin-proteasome pathway. BTK degrader-2 can be used for the study of B-cell-related diseases .
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- HY-162972
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PROTACs
PD-1/PD-L1
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Inflammation/Immunology
Cancer
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PROTAC PD-L1 degrader-2 is a PD-L1 PROTAC degrader with an IC50 of 197.4 nM and a Kd of 301 nM. PROTAC PD-L1 degrader-2 induces PD-L1 endocytosis, drives degradation via the proteasomal and lysosomal pathways, and inhibits the PD-1/PD-L1 interaction. As an immune activator, PROTAC PD-L1 degrader-2 increases the levels of CD4 +, CD8 +, granzyme B and perforin. PROTAC PD-L1 degrader-2 can be used in studies related to colon cancer immunology .
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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-179424
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PROTACs
HIF/HIF Prolyl-Hydroxylase
p38 MAPK
Akt
PI3K
MEK
Apoptosis
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Cancer
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PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and p-AKT expression in the MAPK and PI3K/AKT pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer .
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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-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-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-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-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-143905
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PROTACs
Mps1
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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-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-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-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-174471
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- HY-174225
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- HY-174443
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PROTACs
Epoxide Hydrolase
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Neurological Disease
Inflammation/Immunology
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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-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-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-153938A
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PROTACs
Phosphatase
|
Metabolic Disease
Cancer
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PROTAC PTPN2 degrader-2 TFA is a potent PTPN2 PROTAC degrader with a DC50 of <50 nM. PROTAC PTPN2 degrader-2 TFA is potential for studying cancer or metabolic diseases, such as colon cancer .
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-
- HY-163938A
-
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PROTACs
|
Cancer
|
|
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-145395
-
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PROTACs
|
Cancer
|
|
PROTAC BRD9 Degrader-2 is a BRD9 bifunctional degrader for researching cancer.
|
-
- HY-132194
-
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Estrogen Receptor/ERR
|
Cancer
|
|
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-161750
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
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 .
|
-
- HY-111841
-
|
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SNIPERs
PROTACs
|
Cancer
|
|
PROTAC CRABP-II Degrader-2 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand .
|
-
- HY-168176
-
|
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PROTACs
HDAC
|
Cancer
|
|
HDAC8 ligand 1 is a PROTAC target protein-ligand of PROTAC HDAC8 Degrader-2 (HY-168174) .
|
-
- HY-157805
-
|
|
PROTACs
SARS-CoV
|
Infection
|
|
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 .
|
-
- HY-177389
-
-
- HY-176388
-
-
- HY-163813
-
-
- HY-174473
-
-
- HY-149679
-
|
|
PROTACs
Bacterial
|
Cancer
|
|
PROTAC eDHFR Degrader-2 (compound 7b) is a potent degrader targeting Escherichia coli dihydrofolate reductase (eDHFR), enabling robust degradation of eDHFR-tagged proteins .
|
-
- HY-176804
-
|
|
Ligands for E3 Ligase
|
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) .
|
-
- HY-130850
-
-
- HY-168248
-
-
- HY-W998262
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
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) .
|
-
- HY-162546
-
|
|
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) .
|
-
- HY-181656
-
|
|
Molecular Glues
Glutathione Peroxidase
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
GPX4 degrader-2 is a GPX4 molecular glue degrader and ferroptosis inducer. GPX4 degrader-2 suppresses GPX4 enzyme activity, promotes ubiquitination-dependent proteasomal degradation of GPX4 protein. GPX4 degrader-2 indues ferroptosis, increases lipid ROS and MDA levels, suppresses glutathione levels in cancer cells. GPX4 degrader-2 inhibits cancer cells proliferation and colony formation. GPX4 degrader-2 can be used for the research of colorectal cancer .
|
-
- HY-182051
-
|
|
HDAC
NOD-like Receptor (NLR)
Caspase
Interleukin Related
|
Inflammation/Immunology
|
|
HDAC3 degrader-2 is a selective HDAC3 degrader. HDAC3 degrader-2 inhibits the activation of the NLRP3 inflammasome by degrading HDAC3, thereby reducing the maturation of IL-1β and caspase-1. HDAC3 degrader-2 exhibits anti-inflammatory activity. HDAC3 degrader-2 can be used in research related to endotoxin shock, colitis and gouty arthritis .
|
-
- HY-180989
-
|
|
PROTACs
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
PROTAC PLK1 Degrader-2 (Compound NC1) is a PLK1 PROTAC degrader with an Kd of 6.06 μM. PROTAC PLK1 Degrader-2 significantly inhibits the proliferation of HeLa cells, induces cell cycle arrest and apoptosis. PROTAC PLK1 Degrader-2 exhibits significant anti-tumor activity in a HeLa cell xenograft tumor mouse model. PROTAC PLK1 Degrader-2 can be used for the study of cervical cancer.
|
-
- HY-186021
-
|
|
PROTACs
YAP
|
Cancer
|
|
PROTAC TEAD degrader-2 (Compound 31) is an efficient TEAD1 PROTAC degrader with a DC50 of 0.6 nM. PROTAC TEAD degrader-2 inhibits the YAP/TAZ-TEAD interaction, with a IC50 of 1.8 nM. PROTAC TEAD degrader-2 exhibits significant selective inhibitory activity against YAP-dependent cancer cells and effectively suppresses the transcriptional activity mediated by YAP. PROTAC TEAD degrader-2 can be used for research on mesothelioma and glioma .
|
-
- HY-181143
-
|
|
PROTACs
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
PROTAC Tubulin degrader-2 is a cereblon (CRBN)-dependent α/β-tubulin PROTAC degrader with DC50 values of 1.73 μM and 1.38 μM. PROTAC Tubulin degrader-2 can inhibit cancer cells proliferation and migration. PROTAC Tubulin degrader-2 can induce G2/M arrest, apoptosis, ROS accumulation. PROTAC Tubulin degrader-2 can be used for the research of cancer, such as non-small-cell lung cancer .
|
-
- HY-185121
-
|
|
PROTACs
CDK
Caspase
|
Cancer
|
|
PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 (HY-171826) through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades CDK2/4/6 and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research .
|
-
- HY-181460
-
|
|
HyT
PARP
|
Cancer
|
|
PARP1 degrader-2 (Compound 11e) is a potent, selective PARP1 HYT degrader (DC50: 2.16 μM). PARP1 degrader-2 selectively binds to and degrades PARP1 but not PARP2. PARP1 degrader-2 mediates the degradation of PARP1 via the ubiquitin-proteasome system (UPS). PARP1 degrader-2 exhibits anticancer activity against triple-negative breast cancer and colon cancer (hydrophobic tag: (HY-W022007); PARP1 ligand: (HY-75706); Linker: (HY-W015300)) .
|
-
- HY-181134
-
|
|
PROTACs
|
Cancer
|
|
PROTAC HMGCR Degrader-2 is a HMGCR PROTAC degrader with an IC50 value of 0.25 μM. PROTAC degrades HMGCR-2 in Insig-silenced HepG2 cells with a DC50 of 0.12 μM. PROTAC HMGCR Degrader-2 takes PROTAC HMGCR Degrader-1 (HY-171823) as the oral prodrug. PROTAC HMGCR Degrader-2 degrades HMGCR by the VHL-dependent ubiquitin-proteasome system and reduces cellular cholesterol in HepG2 cells. PROTAC CDK2/4/6 Degrader-2 can be used for hyperlipidemia research .
|
-
- HY-171802
-
|
|
PROTACs
LRRK2
|
Neurological Disease
|
|
PROTAC LRRK2 Degrader-2 is a PROTAC-based degrader targeting LRRK2 with a DC50 of 0.14 nM. PROTAC LRRK2 Degrader-2 recruits LRRK2 or its mutants to the cereblon E3 ubiquitin ligase, thereby mediating the targeted ubiquitination and subsequent proteasomal degradation of LRRK2. PROTAC LRRK2 Degrader-2 can be used in research related to Parkinson's disease .
|
-
- HY-180793
-
|
|
PROTACs
Deubiquitinase
|
Cancer
|
|
PROTAC USP7 Degrader-2 (Compound D16) is an efficient and selective USP7 PROTAC degrader with a DC50 of 1.91 μM (in TE-12 cells). PROTAC USP7 Degrader-2 inhibits the migration of upper gastrointestinal tract (UGI) cancer cells and shows relatively weak anti-proliferative activity. PROTAC USP7 Degrader-2 can be used in the research of metastatic upper gastrointestinal cancer.
|
-
- HY-180967
-
|
|
Bcr-Abl
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC BCR-ABL Degrader-2 is a selective Bcr-Abl T315 PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-Abl T315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research .
|
-
- HY-181537
-
|
|
PROTACs
SNIPERs
YAP
IAP
|
Cancer
|
|
PROTAC TEAD1/IAP degrader-2 is an IAP-harnessing TEAD1 PROTAC degrader, with a DC50 of 170 nM against TEAD1 in NCI-H2052 cells. PROTAC TEAD1/IAP degrader-2 exhibits moderate antiproliferative activity in Hippo pathway-dependent mesothelioma cells. PROTAC TEAD1/IAP degrader-2 inhibits the expression of CTGF, but with a weaker effect than the TEAD inhibitor VT-107 (HY-134957). PROTAC TEAD1/IAP degrader-2 can be used in mesothelioma-related research .
|
-
- HY-164896
-
|
|
PIN1
|
Cancer
|
|
PIN1 degrader-2 (compound 164A10) is a potent and selective covalent PIN1 degrader (IC50 = 4.1 nM) that induces PIN1 degradation in cancer cells (DC50 < 500 nM). PIN1 degrader-2 can be used for cancer research .
|
-
- HY-180972
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
PROTAC EML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. PROTAC EML4-ALK Degrader-2 shows potent selective inhibitory activity to ALK with an IC50 of 1.6 nM. PROTAC EML4-ALK exhibits selectivity over IGF1R, INSR, FLT3, and FGFR2. PROTAC EML4-ALK Degrader-2 shows anti-cancer activities both in vitro and vivo. PROTAC EML4-ALK Degrader-2 can be used for non-small cell lung cancer (NSLC), liver lung and cervical cancer research .
|
-
- HY-186023
-
|
|
Target Protein Ligand-Linker Conjugates
YAP
|
Cancer
|
|
TEAD ligand-Linker Conjugate 1 is a synthetic target protein ligand-linker conjugate that can be used for the synthesis of PROTACs, such as PROTAC TEAD degrader-2 (HY-186021). PROTAC TEAD degrader-2 is a potent TEAD1 PROTAC degrader with anti-cancer activity .
|
-
- HY-180991
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Arg12-AHX is a synthetic E3 ligase-ligand conjugate that can be used for the synthesis of PROTACs, such as PROTAC PLK1 Degrader-2 (HY-180989). PROTAC PLK1 Degrader-2 is a PLK1 PROTAC degrader with anti-tumor activity .
|
-
- HY-182959
-
|
|
Hsp-targeting Chimeras
LYTACs
PD-1/PD-L1
HSP
|
Cancer
|
|
Hsp70TAC PD-1 Degrader-2 is a PD-L1 Hsp70TAC (Hsp70-targeting Chimeras) degrader with Kd values of 0.36 μM. Hsp70TAC PD-1 Degrader-2 forms a ternary complex with Hsp70 and PD-L1 to drive PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 induces degradation of mature membrane-bound PD-L1 in an Hsp70-dependent manner and via caveolin-mediated endocytosis and lysosomal trafficking. Hsp70TAC PD-1 Degrader-2 accumulates preferentially in tumor cells with elevated Hsp70 expression for tumor-selective PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 can be used for the research of cancer, such as breast invasive carcinoma, glioblastoma multiforme, diffuse large b-cell lymphoma . (Pink: PD-1/PD-L1 ligand (HY-19745A); Blue: Hsp70 ligand (HY-182979); Black: linker (HY-182982)).
|
-
- HY-180826
-
-
- HY-W999529
-
-
- HY-181898
-
|
|
PROTACs
IRAK
|
Inflammation/Immunology
|
|
PROTAC IRAK3 degrader-2 (Compound 17) is a IRAK3 PROTAC degrader with a DC50 ≤ 50 nM. It promotes ubiquitination and degradation of IRAK3, and is applicable to the research of immune diseases .
|
-
- HY-179608
-
-
- HY-181261
-
-
- HY-168249
-
|
|
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-164043
-
|
|
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-181539
-
-
- HY-W803227
-
|
|
PROTAC Linkers
|
Cancer
|
|
1-(2-Chloro-acetyl)-piperazine is a PROTAC linker. 1-(2-Chloro-acetyl)-piperazine can be used to synthesize PROTAC TEAD1/IAP degrader-2 (HY-181537) .
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-
- HY-181538
-
-
- HY-158431
-
-
- HY-146369
-
|
|
PROTACs
VEGFR
|
Cancer
|
|
PROTAC VEGFR-2 degrader-2 is a VEGFR-2 (KDR) PROTAC degrader with weak inhibitory activity against VEGFR-2 (IC50 > 1 μM). It is applicable to the research of cancer-related pathological angiogenesis .
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-
- HY-176823
-
|
|
PROTACs
SGK
|
Cancer
|
|
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)) .
|
-
- HY-171334
-
|
|
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 .
|
-
- HY-158429
-
|
|
PROTACs
Cytochrome P450
|
Cancer
|
|
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) .
|
-
- HY-W022007
-
|
JBP
|
Ligands for E3 Ligase
|
Others
|
|
5-Norbornene-2-methylamine (JBP) is a hydrophobic tag. 5-Norbornene-2-methylamine can be used for the synthesis of HyT degraders, such as PARP1 degrader-2 (HY-181460) .
|
-
- HY-162841
-
-
- HY-W761300
-
|
|
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) .
|
-
- 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) .
|
-
- HY-169073
-
|
|
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) .
|
-
- HY-162840
-
|
|
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) .
|
-
- HY-162842
-
-
- HY-186022
-
|
|
Ligands for Target Protein for PROTAC
YAP
|
Cancer
|
|
YAP/TAZ-TEAD-IN-3 is a YAP/TAZ-TEAD interaction inhibitor with an IC50 of 1.8 nM. YAP/TAZ-TEAD-IN-3 can be used as a TEAD1 ligand to construct PROTACs, such as PROTAC TEAD degrader-2 (HY-186021) .
|
-
- HY-163865
-
|
|
PROTACs
|
Cancer
|
|
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 .
|
-
- 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) .
|
-
- HY-180990
-
-
- HY-181900
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
E3 Ligase Ligand-linker Conjugate 226 is a synthetic E3 ligase ligand-linker conjugate that can be used to synthesize PROTACs, such as PROTAC IRAK3 degrader-2 (HY-181898). GXF-111 is a IRAK PROTAC degrader with anti-tumor activity .
|
-
- HY-176335
-
-
- HY-179434
-
-
- HY-169074
-
|
|
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 .
|
-
- HY-112811
-
|
|
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 .
|
-
- HY-161749
-
|
|
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 .
|
-
- HY-176477
-
|
|
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) .
|
-
- HY-128528
-
|
|
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) .
|
-
- HY-161675
-
|
|
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 .
|
-
- HY-182979
-
|
|
HSP
|
Cancer
|
|
HSP70 ligand 2 is an HSP70 ligand and serves as a ligand for PROTAC target proteins. HSP70 ligand 2 can be used to synthesize Hsp70TAC BRD4 Degrader-1 (HY-182958) and Hsp70TAC PD-1 Degrader-2 (HY-182959) .
|
-
- HY-P11631
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Arg12, a 12-amino acid peptide sequence, is an E3 ubiquitin ligase ligand. Arg12 can be used to synthesize PROTACs, such as PROTAC PLK1 Degrader-2 (HY-180989). Arg12 can also act as a cell transmembrane peptide (CPP), facilitating the entire molecule to enter the cell .
|
-
- HY-159006
-
|
|
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) .
|
-
- HY-162545
-
|
|
MAP4K
Ligands for Target Protein for PROTAC
|
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 .
|
-
- HY-186219
-
|
|
Ligands for Target Protein for PROTAC
PIN1
|
Cancer
|
|
PIN1 ligand-3 (Compound I-1) is a PIN1 ligand. PIN1 ligand-3 serves as a Ligand for Target Protein for PROTAC for the synthesis of PIN1 PROTAC degraders, such as PROTAC PIN1 degrader-2 (HY-186218). PIN1 ligand-3 is applicable in cancer research .
|
-
- HY-181899
-
|
|
IRAK
Ligands for Target Protein for PROTAC
|
Inflammation/Immunology
|
|
IRAK3 ligand-3 is a IRAK3 (IRAK-M) ligand. As a Ligand for Target Protein for PROTAC, IRAK3 ligand-3 is used to develop and design degraders of PROTAC IRAK3, such as PROTAC IRAK3 degrader-2 (HY-181898). IRAK3 ligand-3 applies to the research of immune diseases .
|
-
- 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) .
|
-
- HY-170335
-
|
|
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)) .
|
-
- HY-181593
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
IAP ligand-Linker Conjugate 2 is a synthetic target E3 ligase ligand-linker conjugate that can be used for the synthesis of PROTACs, such as PROTAC TEAD1/IAP degrader-3 (HY-181590). PROTAC TEAD degrader-2 is a potent TEAD1/IAP PROTAC degrader with anti-cancer activity .
|
-
- HY-178804
-
|
|
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 .
|
-
- 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) .
|
-
- HY-181852
-
-
- HY-186064
-
-
- HY-130815A
-
-
- HY-130815
-
-
- HY-171823
-
|
|
PROTACs
HMG-CoA Reductase (HMGCR)
|
Metabolic Disease
|
|
PROTAC HMGCR Degrader-1 is an orally active HMGCR PROTAC degrader with IC50 of 1.32 μM. PROTAC HMGCR Degrader-1 is a lactone prodrug of PROTAC HMGCR Degrader-2 (HY-181134). PROTAC HMGCR Degrader-1 achieves high plasma exposure of the active ingredient leading to robust HMGCR degradation and demonstrating promising cholesterol-lowering efficacy in vivo. PROTAC HMGCR Degrader-1 can be used for hyperlipidemia research .
|
-
- HY-171826
-
|
|
CDK
PROTACs
|
Cancer
|
|
PROTAC CDK2/4/6 Degrader-1 is an orally active CDK2/CDK4/CDK6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-1 is a prodrug derived from PROTAC CDK2/4/6 Degrader-2 via one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-1 can be used for malignant melanoma research .
|
-
- 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) .
|
-
- HY-150251
-
|
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) .
|
-
- 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.
|
-
- HY-160533
-
|
|
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 .
|
-
- HY-W1128213
-
|
|
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 .
|
-
- 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-183783
-
|
|
PROTACs
RET
STAT
ERK
Apoptosis
|
Endocrinology
Cancer
|
|
PROTAC RET Degrader 2 is a RET degrader with a target IC50 of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma .
|
-
- HY-182945
-
|
|
Molecular Glues
IKZF Family
HOXA
Interleukin Related
NF-κB
|
Cancer
|
|
IKZF2-degrader 5 is a highly efficient, highly selective, rapidly acting, and orally active IKZF2 molecular glue degrader. IKZF2-degrader 5 induces IKZF2 degradation via the Cullin-CRBN-dependent pathway. IKZF2-degrader 5 promotes the production of pro-inflammatory IL-2. IKZF2-degrader 5 attenuates the immunosuppressive function of regulatory T cells (Tregs). IKZF2-degrader 5 triggers rapid, significant, and sustained IKZF2 degradation in the spleen and thymus of mice. IKZF2-degrader 5 inhibits tumor growth. IKZF2-degrader 5 can be used for the research of B16F melanoma .
|
-
- HY-153322
-
|
|
PROTACs
Itk
|
Inflammation/Immunology
Cancer
|
|
ITK degrader 2 is an orally active ITK PROTAC degrader with a DC50 < 0.001 nM. ITK degrader 2 degrades ITK via the ubiquitin-proteasome pathway. ITK degrader 2 can be used in the research of cancer, autoimmune diseases and inflammatory diseases .
|
-
- HY-163709
-
|
|
PROTACs
FAK
Akt
ERK
|
Cancer
|
|
PROTAC FAK degrader 2 is an orally active PROTAC FAK degrader with a DC50 of 60.10 nM. PROTAC FAK degrader 2 forms a ternary complex with FAK and CRBN E3 ubiquitin ligase, driving proteasome-mediated degradation of total and phosphorylated FAK. PROTAC FAK degrader 2 inhibits phosphorylation of AKT and ERK, suppressing their downstream signaling pathways. PROTAC FAK degrader 2 reduces cancer cell viability, adhesion, migration, and invasion. PROTAC FAK degrader 2 exerts anti-tumor activity in HCT8/T tumor xenografts in mice. PROTAC FAK degrader 2 can be used for the research of breast cancer, colorectal cancer, lung cancer .
|
-
- 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-163818
-
|
|
Histone Methyltransferase
|
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-185300
-
|
|
IKZF Family
Molecular Glues
|
Cancer
|
|
IKZF2-degrader 4 (Page 650, third compound from the top in the right column) is an IKZF2 Molecular glue degrader. IKZF2-degrader 4 degrades IKZF2 protein. IKZF2-degrader 4 can be used in the research of cancer .
|
-
- HY-181972
-
|
|
PROTACs
WDR5
|
Cancer
|
|
PROTAC WDR5 degrader 2 is a WDR5 PROTAC degrader. PROTAC WDR5 degrader 2 induces WDR5 degradation via the ubiquitin-proteasome system by forming a ternary complex with WDR5 and an E3 ligase. PROTAC WDR5 degrader 2 can be used in leukemia-related research .
|
-
- HY-180132
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
PROTAC AURKA degrader 2 (compound D) is a potent and selective PROTAC AURKA degrader with an IC50 of 3.58 nM. PROTAC AURKA degrader 2 exhibits 21.6-fold selectivity for AURKA over AURKB (IC50 = 77.2 nM). PROTAC AURKA degrader 2 specifically depletes AURKA on the mitotic spindle .
|
-
- HY-177780
-
|
|
Molecular Glues
CDK
Apoptosis
|
Cancer
|
|
Cyclin K degrader 2 is a molecular glucose degrading agent that targets the cyclin K protein. Cyclin K degrader 2 has inhibitory activity against CDK1 and CDK9. Cyclin K degrader 2 causes a decrease in RNA polymerase II Ser2 phosphorylation levels, downregulation of DNA damage response gene expression, accumulation of DNA damage, G1 phase arrest of the cell cycle, and apoptosis. Cyclin K degrader 2 can be used for cancer research .
|
-
- HY-161177
-
|
|
PROTACs
SARS-CoV
Virus Protease
|
Infection
|
|
PROTAC KRAS G12D degrader 2 is a peptidomimetic PROTAC specifically targeting the dimeric SARS-CoV-2 3CL Pro protein. PROTAC KRAS G12D degrader 2 inhibits SARS-CoV-2 3CLPro with an IC50 of 21.2 μM. PROTAC KRAS G12D degrader 2 specifically binds to the active site of SARS-CoV-2 3CL Pro. PROTAC KRAS G12D degrader 2 reduces protein levels of SARS-CoV-2 3CL Pro without affecting cell viability. PROTAC KRAS G12D degrader 2 can be used for the study of viral infections in Coronavirus genera .
|
-
- HY-163759
-
|
|
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-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-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-180262
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK6 Degrader 2 (compound 48b), the active form of PROTAC CDK6 Degrader 1 (HY-180277), is a potent and selective PROTAC CDK6 degrader that binds strongly to KLHDC2 (KD = 0.005 μM). PROTAC CDK6 Degrader 2 functions through a KLHDC2-dependent and ubiquitin-proteasome-mediated mechanism. PROTAC CDK6 Degrader 2 can be used for cancer research .
|
-
- HY-176824
-
-
- HY-175527
-
|
|
HyT
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
ALK degrader 2 is an orally active ALK HyT 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)) .
|
-
- 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-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-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-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-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-177754
-
-
- 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-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-45512
-
-
- HY-181973
-
-
- HY-176044
-
-
- HY-171141
-
-
- HY-180263
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
KLHDC2 ligand 4 (compound KL-3 (8)) is an E3 ligase ligand that can be used for synthesis of PROTAC CDK6 Degrader 2 (HY-180262) .
|
-
- HY-181918
-
-
- HY-180264
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
KLHDC2 ligand 4-cyclohexane-CO-pip-cyclobutane is an E3 ubiquitinase ligand-linker conjugate that can be used for synthesis of PROTAC CDK6 Degrader 2 (HY-180262) .
|
-
- HY-W017389S1
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
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 .
|
-
- 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-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
|
|
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)) .
|
-
- HY-176046
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
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) .
|
-
- 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-176125
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
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) .
|
-
- HY-178517
-
|
|
E1/E2/E3 Enzyme
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-C1-O-CO-C11 is a ligand for E3 ubiquitin ligase. Thalidomide-C1-O-CO-C11 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) .
|
-
- HY-183729
-
|
|
Ligands for Target Protein for PROTAC
RET
|
Endocrinology
Cancer
|
|
RET-IN-34 is a RET inhibitor with an IC50 of 0.89 nM. RET-IN-34 serves as a target protein ligand for PROTAC synthesis (Ligand for Target Protein for PROTAC). RET-IN-34 is applicable for the synthesis of PROTAC RET Degrader 2 (HY-183783). RET-IN-34 exhibits anticancer activity against medullary thyroid carcinoma. RET-IN-34 can be used in studies related to medullary thyroid carcinoma .
|
-
- HY-168543
-
|
|
PROTACs
Aurora Kinase
Mps1
|
Cancer
|
|
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) .
|
-
- HY-W670700
-
|
|
MMP
|
Others
|
|
2,5-Dihydroxy-4-methoxyacetophenone (compounds 3) can be isolated from the 80% methanol extract of roots of Cynanchum paniculatum Kitagawa. 2,5-Dihydroxy-4-methoxyacetophenone inhibits glutamate-induced cytotoxicity in hippocampal HT22 cell line . 2,5-Dihydroxy-4-methoxyacetophenone significantly inhibites MMP-13 expression in SW1353 cells, and have the potential for alleviating cartilage degradation .
|
-
- HY-178518
-
|
|
E3 Ligase Ligand-Linker Conjugates
E1/E2/E3 Enzyme
|
Cancer
|
|
Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine is an E3 ligase ligand-linker conjugate containing a cereblon (CRBN) ligand for E3 ubiquitin ligase and a linker. Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine can be used to synthesize PROTAC CDK4/6/9 degrader 2 (HY-178516) .
|
-
- HY-159651
-
|
|
PROTACs
17β-HSD
|
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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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-180989
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PROTACs
Polo-like Kinase (PLK)
Apoptosis
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Cancer
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PROTAC PLK1 Degrader-2 (Compound NC1) is a PLK1 PROTAC degrader with an Kd of 6.06 μM. PROTAC PLK1 Degrader-2 significantly inhibits the proliferation of HeLa cells, induces cell cycle arrest and apoptosis. PROTAC PLK1 Degrader-2 exhibits significant anti-tumor activity in a HeLa cell xenograft tumor mouse model. PROTAC PLK1 Degrader-2 can be used for the study of cervical cancer.
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- HY-180991
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Arg12-AHX is a synthetic E3 ligase-ligand conjugate that can be used for the synthesis of PROTACs, such as PROTAC PLK1 Degrader-2 (HY-180989). PROTAC PLK1 Degrader-2 is a PLK1 PROTAC degrader with anti-tumor activity .
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- HY-180990
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- HY-P11631
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Ligands for E3 Ligase
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Cancer
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Arg12, a 12-amino acid peptide sequence, is an E3 ubiquitin ligase ligand. Arg12 can be used to synthesize PROTACs, such as PROTAC PLK1 Degrader-2 (HY-180989). Arg12 can also act as a cell transmembrane peptide (CPP), facilitating the entire molecule to enter the cell .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
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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| Cat. No. |
Product Name |
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Classification |
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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-133139
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Azide
PROTAC Synthesis
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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-153023
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PROTAC Synthesis
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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-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-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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- 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-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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