Search Result
Results for "
Degrader-1
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-149678
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PROTACs
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Cancer
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PROTAC eDHFR Degrader-1 is a PROTAC that is effective degradation of eDHFR-YFP, various POIs-including YFP and Luciferase [1].
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- HY-147108
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Mitochondrial Metabolism
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Mitochondria degrader-1 (example 5) is a potent mitochondria degrader. Mitochondria degrader-1 induces the degradation of the injured mitochondria by the autophagy mechanism. Mitochondria degrader-1 can be used for the research of neurodegenerative disease, cancer, inflammatory disease, age-related disease, metabolic disease, mitochondrial disease or Down's disease [1].
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- HY-156591
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PROTACs
Mixed Lineage Kinase
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Others
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PROTAC MLKL Degrader-1 (Compound 36) is a PROTAC degrader of MLKL, with a Dmax ＞90%. PROTAC MLKL Degrader-1 contains modified CRBN ligands, linker and Lenalidomide (HY-A0003)-linker fragments. PROTAC MLKL Degrader-1 abrogates cell death in a TSZ model of necroptosis.
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- HY-153880
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PROTACs
Ras
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Cancer
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KRAS degrader-1 (compound 1) is a potent KRAS degrader. KRAS degrader-1 target specific proteins for degradation through the autophagy-lysosomal degradation pathway [1].
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- HY-163295
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ADC Cytotoxin
Btk
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Cancer
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BTK degrader-1 (compound 1) is a Bruton’s tyrosine kinase (BTK) bifunctional degrader that can be conjugated with CD79b. BTK degrader-1 (compound 1) has anti-tumor effect [1].
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- HY-168530
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PD-1/PD-L1
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Cancer
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PDL1 degrader-1 (compound PMT-O9-1A) is a potent PD-L1 degrader. PDL1 degrader-1 decreases the protein expression of PD-L1. PDL1 degrader-1 shows cytotoxicity. PDL1 degrader-1 shows anticancer activity [1].
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- HY-163641
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Molecular Glues
Androgen Receptor
E1/E2/E3 Enzyme
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Cancer
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AR Degrader-1 (Compound ML 2-9) is a molecular glue androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR through DCAF16 (E3 ligase) without obvious cytotoxicity in LNCaP prostate cancer cells [1].
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- HY-147656
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ATTECs
NAMPT
Autophagy
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Cancer
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NAMPT degrader-1 (Compound A3), an autophagosome-tethering compound (ATTEC), is an nicotinamide phosphoribosyltransferase (NAMPT) degrader with an IC50 of 0.023 μM. NAMPT degrader-1 significantly induces the degradation of NAMPT through the autophagy-lysosomal pathway and shows excellent cellular antitumor potency [1].
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- HY-162331
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Molecular Glues
STING
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Inflammation/Immunology
Cancer
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STING Degrader-1 (compound 2), a molecular glue, is a potent STING degrader that covalently binds to STING and E3 ligase. STING Degrader-1 exhibits a "hook effect", that degrades 75% STING protein at 10 μM, and degrades ca. 30% STING protein at 30 μM [1].
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- HY-162679
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c-Met/HGFR
Apoptosis
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Cancer
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c-Met degrader-1 (Compound H11) is an orally active c-Met degrader (through the ubiquitin proteasome system). c-Met degrader-1 has anti-hepatocellular carcinoma activity (HCC) and inhibits tumor growth in MHCC97H xenografts. c-Met degrader-1 inhibits HCC cell growth, arrests cell cycle, and induces apoptosis. c-Met degrader-1 may overcome resistance to type Ib inhibitors [1].
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- HY-112098
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PROTACs
Estrogen Receptor/ERR
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Cancer
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PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
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- HY-147048
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STAT
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Cancer
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STAT3 degrader-1 (compound 295) is a potent STAT3 degrader. STAT3 degrader-1 can be used for researching anticancer [1]. STAT3 degrader-1 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-156152A
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Histone Methyltransferase
PROTACs
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Cancer
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CARM1 degrader-1 hydrochloride is the hydrochloride salt form of CARM1 degrader-1 (HY-156152). CARM1 degrader-1 hydrochloride is a PROTAC degrader for co-activator associated argininemethyltransferase 1 (CARM1), which degrades CARM1 in a VHL- and proteasome-dependent manner with a DC50 of 8.1 nM. CARM1 degrader-1 hydrochloride inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, and thus inhibits breast cancer cell migration [1].
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- HY-161110
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Amyloid-β
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Neurological Disease
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APP degrader-1 (Compound 0152) is an orally active amyloid precursor protein (APP) degrader that induces APP degradation and reduces the extracellular release of Aβ42. APP degrader-1 can bind to both CAPRIN1 and APP, and enhances their interaction as well as CAPRIN1-mediated APP degradation through the endosome-lysosome pathway [1].
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- HY-162014
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PROTACs
WDR5
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Cancer
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WDR5 degrader-1 (compound 25) is a cereblon (CRBN)-recruiting WDR5 degrader. WDR5 degrader-1 selectively degraded WDR5 over the CRBN neo-substrate IKZF1 [1].
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- HY-115865
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IAP
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Cancer
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XIAP degrader-1, a primary amine tethered small molecule, promotes the degradation of X-linked inhibitor of apoptosis protein (XIAP).
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- HY-128838A
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Estrogen Receptor/ERR
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Others
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(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1. PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader .
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- HY-128838
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PROTACs
Estrogen Receptor/ERR
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Cancer
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PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader .
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- HY-157216
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HDAC
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Cancer
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HDAC1 Degrader-1 (compound 1a) is an HDAC1 degrader with anticancer activity. HDAC1 Degrader-1 significantly reduces HDAC1 levels in MM.1S multiple myeloma cells [1].
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- HY-173369
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MAGL
Ligands for E3 Ligase
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Cancer
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PROTAC MAGL degrader-1 is an orally active PROTAC agent that simultaneously targets monoacylglycerol lipase (MAGL) and E3 ubiquitin ligase MDM2. PROTAC MAGL degrader-1 degrades MAGL and inhibits the binding of MDM2 to p53. PROTAC MAGL degrader-1 can partially penetrate the blood-brain barrier (BBB). PROTAC MAGL degrader-1 induces glioblastoma stem cells (GSCs) apoptosis. (E3 ligase ligand: HY-128837; target protein ligand + linker: HY-173370; target protein inhibitor: HY-15249) [1].
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- HY-176451
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CDK
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Cancer
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CDK9 degrader-1 (Compound AZ-9) is a selective CDK9 degrader (DC50: 0.4073 µM). CDK9 degrader-1 recruits ATG101 to initiate the autophagy-lysosome pathway and forms autophagosomes by recruiting LC3, which then fuses with lysosomes to degrade CDK9 and its partner protein Cyclin T1 (DC50: 1.215 µM). CDK9 degrader-1 induces caspase 3-mediated apoptosis. CDK9 degrader-1 has antitumor activity in a mouse HCT116 xenograft model [1].
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- HY-134725
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- HY-164895
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PIN1
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Cancer
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PIN1 degrader-1 (Compound 158H9) is the inhibitor for proline cis trans isomerase (Pin1) with an IC50 of 21.5 nM. PIN1 degrader-1 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation. PIN1 degrader-1 inhibits the cell viability of multi cancer cells, and can be used in cancer research [1].
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- HY-147654
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PROTACs
Influenza Virus
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Infection
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PROTAC Hemagglutinin Degrader-1 (Compound V3) is a potent PROTAC influenza hemagglutinin (HA) degrader with a median degradation concentration of 1.44 μM. PROTAC Hemagglutinin Degrader-1 shows broad-spectrum anti-influenza virus activity [1].
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- HY-145159
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SHP2
PROTACs
Phosphatase
Apoptosis
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Cancer
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SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases [1].
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- HY-163638
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- HY-147943
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PROTACs
Btk
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Cancer
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PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth [1]. PROTAC BTK Degrader-1 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-150608
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PROTACs
STING
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Inflammation/Immunology
Cancer
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PROTAC STING Degrader-1 is a PROTAC degrader targeting the STING pathway with a DC50 of 3.2 μM. PROTAC STING Degrader-1 exerts high anti-inflammatory efficacy. PROTAC STING Degrader-1 can be used to study diseases such as acute kidney injury and inflammatory bowel diseases (IBDs). (Pink: STING ligand (HY-138682); Blue: CRBN ligand (HY-10984); Black: linker (HY-W015883)) [1] .
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- HY-130614
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PROTACs
Histone Methyltransferase
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Cancer
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PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit [1].
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- HY-157764
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PROTACs
ATM/ATR
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Cancer
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PROTAC ATR degrader-1 (compound ZS-7) is a potent PROTAC degrader of ataxia telangiectasia and Rad3-related (ATR), with DC50 of 0.53 μM. PROTAC ATR degrader-1 plays an importnt role in cancer research [1].
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- HY-153864
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PROTACs
MEK
ERK
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Cancer
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PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells [1].
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- HY-145737
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PROTACs
Ras
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Cancer
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PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity [1].
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- HY-156152
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Histone Methyltransferase
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Cancer
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PROTAC CARM1 degrader-1 (compound 3b) is a degrader (DC50=8.1 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-1 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration [1].
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- HY-161749
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PROTACs
Anaplastic lymphoma kinase (ALK)
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Cancer
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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 [1].
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- HY-153415
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PROTACs
Bcr-Abl
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Cancer
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PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoethyl linker. PROTAC BCR-ABL Degrader-1 induces Bcr-Abl degradation in a ubiquitinproteasom-dependent manner. PROTAC BCR-ABL Degrader-1 exhibits antiproliferative activity against K562 cells, and has the potential to study cancer [1].
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- HY-148691
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Phosphatase
PROTACs
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Metabolic Disease
Cancer
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PROTAC PTPN2 degrader-1 (compound example 77) is a potent PTPN2 degrader. PROTAC PTPN2 degrader-1 has the potential for the research of cancer or metabolic disease [1].
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- HY-173320
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Wee1
HSP
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Cancer
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HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker) [1].
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- HY-153424
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Target Protein Ligand-Linker Conjugates
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Cancer
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PROTAC SMARCA2 degrader-1 (compound ex7) is a BRM2 (SMARCA2) degrader (DC50<0.1 μM). PROTAC SMARCA2 degrader-1 is also an E3 ubiquitin ligase binding linker useful in research of cancers. PROTAC SMARCA2 degrader-1 is a target protein ligand-linker conjugate [1].
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- HY-155552
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Molecular Glues
Apoptosis
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Cancer
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GSPT1 degrader-1 (compound 9q) is a potent degrader of G1 to S phase transition 1 (GSPT1) via ubiquitin-proteasome system, serves as one of Molecular Glues. GSPT1 degrader-1 also induces cell G0/G1 phase arrest and apoptosis [1].
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- HY-160525
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Molecular Glues
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Cancer
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CDO1 degrader-1 (compound 8) is a molecular glue degrader that targets cysteine dioxygenase (CDO1) [1].
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- HY-160532
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Casein Kinase
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Cancer
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CK1α degrader-1 (Compound 82) is an orally active CK1α degrader with a DC50 of 0.105 μM. CK1α degrader-1 can be used for the research of cancer [1].
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- HY-158345
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PROTACs
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Cancer
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PROTAC VHL-type degrader-1 (compound 9b) is a VHL-type PROTAC degrader. PROTAC VHL-type degrader-1 induces ATM degradation synergistically enhancing the efficacy of ATR inhibitor AZD6738 [1].
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- HY-172208
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PROTACs
Cyclic GMP-AMP Synthase
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Inflammation/Immunology
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PROTAC cGAS degrader-1 (Compound TH35) is an effective and selective cGAS PROTAC degrader, with DC50 values of 0.9 μM and 4.6 μM in THP-1 and RAW 264.7 cells, respectively. PROTAC cGAS degrader-1 can inhibit the activation of cGAS signaling induced by dsDNA. PROTAC cGAS degrader-1 has anti-inflammatory activity and can be used in the research of cGAS-related inflammatory diseases. (Pink: cGAS inhibitor (HY-133916); Black: Linker (HY-W411604); Blue: E3 ligase ligand (HY-43722)) [1]
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- HY-163851
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PROTACs
HIV
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Infection
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PROTAC Vif degrader-1 (Compound L15) is a Vif PROTAC degrader. PROTAC Vif degrader-1 has antiviral activity against HIV-1 (EC50: 33.35 μM against HIV-1IIIB). Blue: CRBN ligand (HY-10984); Black: linker; Pink: HIV-1 inhibitor(HY-163852) [1].
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- HY-163440
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PROTACs
NAMPT
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Cancer
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PROTAC NAMPT Degrader-1 is a potent PROTAC targeting NAMPT with aDC50 value of 217 nM. PROTAC NAMPT Degrader-1 has anti-proliferative activity with an IC50 value of 0.12μM against A2780 cells.
(Structure Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker) [1].
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- HY-143904
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PROTACs
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Cancer
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PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells [1].
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- HY-161108
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PROTACs
Checkpoint Kinase (Chk)
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Cancer
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PROTAC Chk1 degrader-1 (Compound PROTAC-2 ) is a potent PROTAC-targeted degrader of Chk1 with a DC50 of 1.33 μM. PROTAC Chk1 degrader-1 can be used in cancer research [1].
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- HY-111844
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PROTACs
SNIPERs
RAR/RXR
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Neurological Disease
Metabolic Disease
Cancer
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PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)) [1] .
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- HY-163372
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MAP4K
PROTACs
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Cancer
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PROTAC HPK1 Degrader-1 (Compound B1) is a potent HPK1 degrader with DC50 value of 1.8 nM. PROTAC HPK1 Degrader-1 inhibits phosphorylation of the SLP76 protein with IC50 value of 496.1 nM. PROTAC HPK1 Degrader-1 is a bona fide HPK1-PROTAC degrader, which provided a potential tool for further HPK1 investigation in TCR signaling [1].
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- HY-158045
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PROTACs
PARP
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Inflammation/Immunology
Cancer
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PROTAC PARP1 degrader-1 (Compound CN0) is a PROTAC degrader of PARP1. PROTAC PARP1 degrader-1 activates the cGAS/STING immunity pathway and eventually enhances T cell killing of tumor cells. PROTAC PARP1 degrader-1 inhibits DNA damage repair, resulting in highly efficient accumulation of cytosolic DNA fragments (Blue: CRBN ligand, Black: linker; Pink: PARP1 inhibitor) [1].
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- HY-D2336
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PROTACs
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Cancer
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PROTAC Aster-A degrader-1 (compound NGF3) is a degrader of the sterol transport protein Aster-A. PROTAC Aster-A degrader-1 can be used as a fluorescence probe. (Red: Aster-A inhibitor, black: linker, Blue: E3 ligase ligand) [1].
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- HY-129523
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PROTACs
Ras
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Cancer
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PROTAC K-Ras Degrader-1 (Compound 518) is a PROTAC. PROTAC K-Ras Degrader-1 can effectively degrades K-Ras based on Cereblon E3 ligand, exhibits ≥70% degradation efficacy in SW1573 cells [1].
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- HY-156244
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PROTACs
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Cancer
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PROTAC GDI2 Degrader-1 (compound 21) is a potent PROTAC GDI2 degrader. PROTAC GDI2 Degrader-1 exhibits excellent in vivo antitumor activity in the GDI2-overexpressing pancreatic xenograft models [1].
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- HY-173560
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ATTECs
SHP2
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Cancer
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SHP2 ATTEC degrader-1 is a SHP2 ATTEC degrader. SHP2 ATTEC degrader-1 has degradation rate of 83.31 at 1.0 μM for 24 h in the PANC-1 cell line. SHP2 ATTEC degrader-1 inhibits cell growth in vivo and in vitro. SHP2 ATTEC degrader-1 induces apoptosis and increases the expression of the epithelial marker ( E-cadherin)， and reduces the expression of interstitial markers (such as N-cadherin, Vimentin) (Pink: LC3 ligand (HY-174085); Black :linker HY-140468; Blue: SHP2 ligand (HY-174084) [1].
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- HY-163897
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PROTACs
Ferroptosis
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Inflammation/Immunology
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PROTAC NCOA4 degrader-1 (Compound V3) is a PROTAC NCOA4 degrader (DC50: 3 nM in HeLa cells). PROTAC NCOA4 degrader-1 is a ferroptosis inhibitor. PROTAC NCOA4 degrader-1 reduces NCOA4 levels and downregulates intracellular ferrous iron (Fe 2+) levels. PROTAC NCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model. (Red: NCOA4 ligand (HY-149457). Black: linker (HY-163903). Blue: VHL ligand (HY-138678B)) [1].
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- HY-169008
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PROTACs
Acetyl-CoA Carboxylase
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Infection
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PROTAC ACC degrader-1 (Compound 9b) is a Acetyl-CoA Carboxylase degrader. PROTAC ACC degrader-1 exhibits superior potency against Aphis craccivora (IC50 = 107.8 μg/mL). (Structure Note: Pink, Target protein ligand (HY-169009); Blue, E3 ligand (HY-10984); Black, linker (HY-W007559) [1].
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- HY-174428
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JAK
STAT
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Cancer
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PROTAC JAK2 degrader-1 (Compound 10i) is a JAK2 PROTAC degrader with a DC50 of 27.35 nM for JAK2 V617F. PROTAC JAK2 degrader-1 promotes the ubiquitination and degradation of JAK2. PROTAC JAK2 degrader-1 inhibits the phosphorylation of JAK2, STAT3 and STAT5. PROTAC JAK2 degrader-1 can be used in the research of myeloproliferative neoplasms (Pink: JAK2 ligand (HY-174430); Blue: E3 ligase ligand (HY-W087383); Black: E3 ligase ligand + linker (HY-174432)) [1].
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- HY-155816
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PROTACs
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Cancer
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PROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SET domain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP.
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- HY-133131
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression [1].
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- HY-168057
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PROTACs
CDK
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Cancer
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PROTAC CDK2 Degrader-1 (Compound 41) is a PROTAC degrader for cyclin-dependent kinase 2 (CDK2). PROTAC CDK2 Degrader-1 inhibits the phosphorylation of RB protein in CDK2 dependent cell line OVCAR3 with an IC50 of 100-500 nM [1].
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- HY-173135
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PROTACs
Histone Demethylase
Apoptosis
|
Cancer
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PROTAC KDM4 degrader-1 (Compound 11) is a KDM4-targeted proteolysis targeting chimeras (PROTAC) degrader. PROTAC KDM4 degrader-1 can degrade KDM4A-C while sparing KDM4D. PROTAC KDM4 degrader-1 exhibits potent antiproliferative activity in esophageal cancer cells. PROTAC KDM4 degrader-1 induces apoptosis and cell cycle arrest, and inhibits histone H3 lysine demethylation. (Blue: E3 ligase ligand (HY-112078), Black: linker (HY-W013381); Pink: ligand for target protein (HY-173136) ) [1].
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- HY-145737A
-
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PROTACs
Ras
|
Cancer
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PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity [1].
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-
- HY-155643
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PROTACs
Glutaminase
|
Cancer
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PROTAC TG2 degrader-1 (compound 11) is a von Hippel-Lindau (VHL)-based PROTAC targeting tissue transglutaminase (TG2) with a KD of 68.9 μM. PROTAC TG2 degrader-1 reduces TG2 in ovarian cancer cells in a proteasome-dependent manner [1].
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-
- HY-103633
-
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PROTACs
Epigenetic Reader Domain
|
Cancer
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PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
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-
- HY-160115
-
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DNA/RNA Synthesis
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Neurological Disease
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TDP-43 degrader-1 (example 3) reduces the TDP-43 aggregation that can be in the research of Amyotrophic lateral sclerosis and? Alzheimer's disease [1].
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- HY-168037
-
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PROTACs
PIN1
|
Cancer
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|
PROTAC PIN1 degrader-1 (compound D4) is a PROTAC targeting PIN1, with a DC50=1.8 nM. The GI50 of PROTAC PIN1 degrader-1 to MDA-MB-468 is >30 μM. PROTAC PIN1 degrader-1 is composed of target protein ligand PIN1 ligand-1 (HY-168038) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part), and PROTAC linker (black part) [1] .
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- HY-163152
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- HY-168593
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β-catenin
PROTACs
Wnt
Histone Demethylase
|
Cancer
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PROTAC KDM3 degrader-1 (Compound 4) is a CRBN-recruiting PROTAC designed based on the IOX1 (HY-12304) scaffold. PROTAC KDM3 degrader-1 selectively degrades the KDM3A and KDM3B proteins, thereby inhibiting the Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 significantly suppresses the self-renewal capacity of colorectal cancer stem cells and inhibits the growth of colorectal cancer tumors. PROTAC KDM3 degrader-1 is suitable for research on colorectal cancer (Target protein ligand (Pink): HY-12304; linker (Black): HY-22335; Conjugate of E3 ligase ligand and linker: HY-112599; E3 ligase (Blue): HY-41547) [1].
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- HY-103628
-
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PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.
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-
- HY-176428
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PROTACs
MNK
Apoptosis
Eukaryotic Initiation Factor (eIF)
|
Cancer
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PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM, and a Dmax > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC50: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety [1]. Pink: MNK1 ligand (HY-176429); Blue: CRBN ligase ligand (HY-A0003); Black: linker (HY-Y1139); CRBN + linker: HY-176430
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-
- HY-125877
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PROTACs
Bcl-2 Family
|
Cancer
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PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM [1].
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- HY-170669
-
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PROTACs
CRM1
Apoptosis
NF-κB
|
Cancer
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|
PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673)) [1].
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-
- HY-155008
-
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PROTACs
Hexokinase
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Cancer
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|
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research [1].
|
-
- HY-146324
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PROTACs
CaMK
Apoptosis
|
Cancer
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PROTAC eEF2K degrader-1 (Compound 11l) is an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells. PROTAC eEF2K degrader-1 mediates eEF2K degradation .
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- HY-156401
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PROTACs
Epigenetic Reader Domain
|
Cancer
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|
BRD9 c-1 (Compound 13-7) is a PROTAC BRD9 degrader . BRD9 Degrader-1 has a micromolar binding affinity for BRD9 and a nanomolar affinity for the BRD9-VCB ternary complex. BRD9 Degrader-1 induces BRD9 proteasome degradation in HEK293T cells, which can be reversed by MLN4924 (HY-70062). (Blue: VH032-cyclopropane-F (HY-125905); Black: linker (HY-W763939); Pink: HY-168695) [1].
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- HY-111840
-
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SNIPERs
PROTACs
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Cancer
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PROTAC CRABP-II Degrader-1 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand [1].
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- HY-131188
-
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PROTACs
Bcl-2 Family
|
Cancer
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PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL (Bcl-2 family member) ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively [1].
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-
- HY-138536
-
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines [1].
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- HY-149845
-
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GSK-3
PROTACs
|
Neurological Disease
|
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PROTAC GSK-3β Degrader-1 (compound 1) is a degrader targets GSK-3β degradation with an IC50 value of 833 nM. PROTAC GSK-3β Degrader-1 contains SB-216763 (a GSK-3β inhibitor), a PEG linker and a CRBN (E3 ligase liand). PROTAC GSK-3β Degrader-1 reduces the neurotoxicity induced by Aβ25-35 peptide and CuSO4. PROTAC GSK-3β Degrader-1 can be used to research in Alzheimer's disease [1].
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- HY-128840
-
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PROTACs
MDM-2/p53
|
Cancer
|
|
PROTAC MDM2 Degrader-1 (Compound 15a) is a MDM2 PROTAC degrader. The structures of both Linker ends of PROTAC MDM2 Degrader-1 are MDM2 ligands. PROTAC MDM2 Degrader-1 can not only block the binding of p53-MDM2, but also degrade the target MDM2 protein by utilizing the function of the E3 ligase of MDM2 itself, thus exerting an anti-tumor effect. (Pink: MDM2 ligand 2 (HY-128836); Black: Linker (HY-128844); Blue: E3 ligase Ligand 15 (HY-128836)) [1]
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- HY-153881
-
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Ras
|
Cancer
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KRAS G12C degrader-1 (Compound 283) is a potent KRAS G12C degrader (DC50: < 100 nM) for cancer research. KRAS G12C degrader-1 is a chaperone (HSP90)-mediated protein degrader (CHAMPs) [1].
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- HY-168641
-
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PROTACs
Apoptosis
HIF/HIF Prolyl-Hydroxylase
|
Cancer
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|
PROTAC HIF-1α degrader-1 (compound V2) is a potent hypoxia-inducible factor-1α (HIF-1α) PROTAC degrader with an IC50 value of 7.54 µM. PROTAC HIF-1α degrader-1 shows anti-proliferative activity. PROTAC HIF-1α degrader-1 decreases the HIF-1α protein expression. PROTAC HIF-1α degrader-1 induces apoptosis. (Pink: ligand for target protein (HY-111387); black: linker (HY-W013731); Blue: E3 ligase ligand (HY-112078)) [1].
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- HY-163920
-
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PROTACs
HDAC
|
Cancer
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|
Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC50 of 0.27 nM in A549 cells [1].
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-
- HY-158985A
-
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Autophagy
AUTACs
|
Cancer
|
|
Amino-PEG3-2G degrader-1 hydrochloride is the hydrochloride salt form of Amino-PEG3-2G degrader-1 (HY-158985). Amino-PEG3-2G degrader-1 hydrochloride is a conjugate of a PEG Linker and a pyrazole-linked FBnG tag for ubiquitin-proteasome system (UPS) induction. Amino-PEG3-2G degrader-1 hydrochloride can be used to synthesize autophagy-targeting chimeras (AUTACs) [1].
|
-
- HY-168135
-
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PROTACs
c-Met/HGFR
|
Cancer
|
|
PROTAC c-Met degrader-1 (Compound Met-DD4) is an orally active PROTAC degrader for c-Met with a DC50 of 6.21 nM. PROTAC c-Met degrader-1 inhibits the proliferation of c-Met-addicted cell MKN-45 with an IC50 of 4.37 nM, and arrests the cell cycle at G0/G1 phase. PROTAC c-Met degrader-1 exhibits antitumor efficacy in MKN-45 xenograft mouse models [1]. (Pink: Ligand for target protein (HY-13404); Blue: Ligand for E3 ligase (HY-W087383); Black: Linker (HY-W074901))
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-
- HY-176489
-
|
|
PROTACs
Ras
|
Cancer
|
|
PROTAC pan-KRAS degrader-1 is a pan-KRAS PROTAC degrader for degrading different KRAS mutation types, such as G12D, G12C, G12V, and G13D. PROTAC pan-KRAS degrader-1 potently degrades KRAS mutation (G12D) in AGS cells, with a DC50 of 1.1 nM, Dmax of 95%. PROTAC pan-KRAS degrader-1 can be used to search diseases caused by KRAS mutation or amplification, especially cancers such as breast cancer, bladder cancer, gastric cancer, etc [1]. Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligase ligand (HY-170353); Black: linker (HY-176491);
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-
- HY-144657
-
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PROTACs
Ras
|
Cancer
|
|
(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo [1].
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-
- HY-131911
-
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PROTACs
Indoleamine 2,3-Dioxygenase (IDO)
|
Inflammation/Immunology
|
|
PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to Cereblon E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells [1].
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-
- HY-129966
-
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PROTACs
IRAK
|
Cancer
|
|
PROTAC IRAK4 degrader-1 (compound I-210) is a Cereblon-based IRAK4 PROTAC. PROTAC IRAK4 degrader-1 is composed of IRAK4 ligand (red part) PROTAC IRAK4 ligand-1 (HY-129967), E3 ligase ligand (blue part) Pomalidomide (HY-10984), and PROTAC linker (black part) AM-Imidazole-PA-Boc (HY-129968) [1].
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-
- HY-163938
-
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PROTACs
|
Cancer
|
|
PROTAC erf3a Degrader-1 (Compound C63) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-1 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-1 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: CRBN ligand (HY-41547)) [1].
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- HY-160262
-
-
- HY-145071
-
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PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Y537S degrader-1 comprises a ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Y537S degrader-1 extracts from patent WO2021143822, example 12. PROTAC ERα Y537S degrader-1 is an estrogen receptor-alpha (ERα) Y537S degrader .
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- HY-158342
-
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PROTACs
YAP
|
Cancer
|
|
PROTAC TEAD degrader-1 (Compound 27) is a PROTAC degrader for transcriptional enhanced associate domain (TEAD). PROTAC TEAD degrader-1 selectively degrades the Flag TEAD2 in a ubiquitin proteasome-dependent manner, with a DC50 of 54.1 nM in 293T cells, inhibits proliferation of NF2-deficient NCI-H226 with an IC50 of 0.21 μM, and regulates expressions of yes associated protein (YAP) target genes. (Pink: TEAD ligand (HY-158400); Black: linker (HY-W008474); Blue: E3 ligase ligand (HY-W087383)) [1]
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- HY-149236
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-
- HY-103636
-
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Sirtuin
PROTACs
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Cancer
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|
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM) [1].
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- HY-130709
-
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PROTACs
CDK
|
Cancer
|
|
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand [1].
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- HY-145479
-
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PROTACs
Androgen Receptor
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Cancer
|
|
PROTAC AR-V7 degrader-1 is an orally active and selective AR-V7 PROTAC degrader with a DC50 of 0.32 μM (in 22Rv1 cells). PROTAC AR-V7 degrader-1 can inhibit the proliferation of tumor cells and exhibit anti-tumor activity. PROTAC AR-V7 degrader-1 can be used for the research of cancers such as prostate cancer [1].(Pink: VPC-14228 (HY-117669); Black: linker (HY-W041652); Blue: VHL Ligand (HY-112078))
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- HY-163757
-
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PROTACs
PD-1/PD-L1
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Inflammation/Immunology
Cancer
|
PROTAC PD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC50 of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer. (Blue: CRBN ligand (HY-150839), Black: linker; Pink: PD-L inhibitor (HY-19745)) [1].
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- HY-176184
-
-
- HY-168016
-
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PROTACs
YAP
|
Cancer
|
|
PROTAC YAP degrader-1 (compound YZ-6) is a PROTAC targeting YAP and also inhibits the nuclear localization of YAP. PROTAC YAP degrader-1 is composed of PROTAC target protein ligand NSC682769 (HY-168017) (red part) and E3 ubiquitin ligase ligand + Linker conjugate (R,S,R)-AHPC-PEG2-C2-boc (HY-168019) (blue+black part), in which the PROTAC Linker used is Acid-PEG2-C2-Boc (HY-140480) and the target protein ligand activity control is Demethyl-NSC682769 (HY-168018) [1] .
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- HY-148521
-
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CDK
FLT3
PROTACs
Apoptosis
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Cancer
|
|
PROTAC FLT3/CDK9 degrader-1 is a potent FLT3 and CDK9 dual PROTAC degrader. PROTAC FLT3/CDK9 degrader-1 induces apoptosis and effective degradation of target proteins FLT3 and CDK9. PROTAC FLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML [1].
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- HY-159609
-
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PROTACs
|
Cancer
|
|
PROTAC GSPT1 degrader-1 (Compound F) is a PROTAC degrader for G1 to S phase transition protein 1 (GSPT1) that degrades GSPT1 with a rate of 95% (1 μM) GSPT1 and 86% (0.1 μM). PROTAC GSPT1 degrader-1 inhibits the cell viability of HL-60 with an IC50 of 9.2 nM. (Pink: ligand for target protein (HY-W599025); Black: linker (HY-159619); Blue: ligand for E3 ligase (HY-W087383)) [1]
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-
- HY-170995
-
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PROTACs
ROR
Apoptosis
|
Cancer
|
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PROTAC ROR1 degrader-1 (Compound 11d) is a PROTAC degrader for pseudokinase ROR1 that degrades ROR1 in NSCLC cells with a DC50s of 40-80 nM. PROTAC ROR1 degrader-1 causes the cleavage of PARP and induces apoptosis in NCI-H23 [1]. (Pink: ligand for target protein ROR1 ligand-1 (HY-170996); Black: linker (HY-W014787); Blue: ligand for VHL E3 ligase (S,R,S)-AHPC (HY-125845))
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- HY-168274
-
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PROTACs
Apoptosis
|
Cancer
|
|
PROTAC TRIB2 degrader-1 (Compound 5k) is an effective TRIB2 degrader that selectively induces TRIB2 degradation through the CRBN-dependent ubiquitin-proteasome pathway. PROTAC TRIB2 degrader-1 can inhibit cell proliferation and induce cell apoptosis, and can be used in cancer research. (Target protein ligand (Pink): HY-168275; linker (black): HY-168276; E3 Ligase Ligand-Linker Conjugates: HY-168277; E3 ligase (Blue): HY-W023573) [1].
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- HY-103632
-
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology [1].
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- HY-151110
-
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PROTACs
CDK
|
Cancer
|
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PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research [1].
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- HY-174233
-
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PROTACs
SARS-CoV
Virus Protease
|
Infection
|
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PROTAC SARS-CoV-2 Degrader-1 (Compound LLP019) is a PROTAC degrader targeting the SARS-CoV-2 main protease (MPro) with a DC50 value of 4.7 μM. PROTAC SARS-CoV-2 Degrader-1 induces MPro ubiquitination and proteasomal degradation to inhibit SARS-CoV-2 replication. PROTAC SARS-CoV-2 Degrader-1 is promising for research of COVID-19 and related coronavirus infections. (Pink: DH03 (HY-32717); Black: linker (HY-42149); Blue: Thalidomide-4-O-CH2-COO(t-Bu) (HY-42771) [1].
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- HY-139186
-
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PROTACs
|
Cancer
|
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PROTAC KRAS G12C degrader-1 is a Cereblon-based KRAS G12C PROTAC degrader. PROTAC KRAS G12C degrader-1 induces CRBN/ KRAS G12C dimerization and degrades GFP- KRAS G12C in reporter cells [1].
|
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- HY-158985
-
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AUTACs
Autophagy
|
Cancer
|
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Amino-PEG3-2G degrader-1 (compound ) is a conjugate of a PEG Linker and a pyrazole-linked FBnG tag for ubiquitin-proteasome system (UPS) induction. Amino-PEG3-2G degrader-1 can be used to synthesize autophagy-targeting chimeras (AUTACs) [1].
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-
- HY-144657A
-
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PROTACs
Ras
|
Cancer
|
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(4S)-PROTAC SOS1 degrader-1 (diTFA) is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 (diTFA) decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 (diTFA) significantly inhibits the tumor growth in vivo [1].
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-
- HY-172368
-
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PROTACs
Histone Methyltransferase
IKZF Family
Apoptosis
|
Inflammation/Immunology
Cancer
|
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PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reduces the methylation level of its substrate BAF155. PROTAC CARM1/IKZF3 degrader-1 is the PROTAC degrader for IKZF 1/3 through a CRBN-dependent pathway. PROTAC CARM1/IKZF3 degrader-1 inhibits the expression of MYC protein, thereby inhibiting the proliferation of a variety of multiple myeloma cells. PROTAC CARM1/IKZF3 degrader-1 induces apoptosis in cell H929. PROTAC CARM1/IKZF3 degrader-1 overcomes immunomodulatory drugs (IMiD, such as pomalidomide) resistance. PROTAC CARM1/IKZF3 degrader-1 can be used in cancer and immunology research [1]. (Pink: ligand for target protein CARM1/IKZF3 ligand 1 (HY-172369); Active form of target protein ligand: EZM 2302 (HY-111109); Black: linker (HY-21999); Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride (HY-41547))
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-
- HY-168242
-
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRM/BRG1 degrader-1 (Example 253) is a PROTAC BRM/BRG1 degrader, with DC50 of 10-100 nM for BRM, > 1 μM for BRG1. PROTAC BRM/BRG1 degrader-1 can be used for cancer research. Blue: E3 ligase ligand (HY-168243), black: linker (HY-168244). Red: BRM/BRG1 inhibitor (HY-W539427) [1].
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-
- HY-132998
-
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PROTACs
HDAC
|
Cancer
|
|
HDAC6 degrader-1 (Compound NP8) is the PROTAC degrader for HDAC6 with a DC50 of 3.8 nM in cell MM.1S [1].(Blue: ligand for E3 ligase Pomalidomide (HY-10984); Black: linker (HY-140213); Pink: ligand for target protein Nexturastat A (HY-16699))
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- HY-147525
-
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PROTACs
Histone Methyltransferase
|
Cancer
|
|
PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes [1].
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- HY-158142
-
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PROTACs
JAK
|
Cancer
|
|
PROTAC TYK2 degrader-1 (CPD-155) is a PROTAC targeting degrader to TYK2 with Dmax >60%. (Structure Note: PINK, TYK2 ligand 1 (HY-158340); Blue, VHL ligand Thalidomide (HY-14658); Black, linker)
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-
- HY-130612
-
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|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A [1].
|
-
- HY-163609
-
|
|
PROTACs
Aldose Reductase
|
Cancer
|
|
PROTAC AKR1C3 degrader-1 (compound 5) is a potent AKR1C3 PROTAC degrader. PROTAC AKR1C3 degrader-1 decreases the protein expression of AKR1C3, AKR1C1/2, and ARv7. PROTAC AKR1C3 degrader-1 has the potential for the research of prostate cancer. (Blue:ubiquitin E3 ligase cereblon ligand (HY-A0003), Black: linker (HY-163647); Pink: AKR1C3 inhibitor (HY-163610)) [1].
|
-
- HY-161708
-
|
|
PROTACs
CDK
FLT3
|
Cancer
|
|
PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (DC50 is 18.73 nM for CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1 induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC50s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383)) [1]
|
-
- HY-170869
-
|
|
PROTACs
FGFR
|
Cancer
|
|
PROTAC FGFR1 degrader-1 (compound S2H) is a PROTAC degrader targeting FGFR1, with IC50=26.81 nM and DC50=39.78 nM in KG1a cells. PROTAC FGFR1 degrader-1 is composed of CRBN-type E3 ligase ligand (blue part) Pomalidomide (HY-10984), target protein ligand (red part) FGFR1 ligand-1 (HY-170871), and PROTAC linker (black part) 9-Bromononanoic acid (HY-W007587), in which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 164 (HY-170870) [1].
|
-
- HY-151110A
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research [1].
|
-
- HY-162412
-
|
|
PROTACs
Adrenergic Receptor
Apoptosis
|
Cancer
|
PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) [1].
|
-
- HY-128845
-
|
|
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
|
PROTAC CRBN Degrader-1 (Compound 14a) is a VHL-CRBN heterodimerization PROTAC degrader that achieves a selective degradation of CRBN by binding two E3 ubiquitin ligases (VHL and CRBN) to each other [1]. (Blue: VHL ligand (S,R,S)-AHPC (HY-125845); Pink: CRBN ligand Pomalidomide-C2-NH2 (HY-128846); Black: Linker (HY-128847))
|
-
- HY-157804
-
|
|
PROTACs
SARS-CoV
|
Infection
|
|
PROTAC SARS-CoV-2 Mpro degrader-1 (compound 5) is a PROTAC degrader targeting the major SARS-CoV-2 protease with broad-spectrum antiviral activity [1].
|
-
- HY-137487
-
|
|
PROTACs
Raf
|
Cancer
|
|
PROTAC BRAF-V600E degrader-1 (compound 23) is a potent PROTAC BRAF-V600E degrader whlie no degradation activity against BRAF-WT. PROTAC BRAF-V600E degrader-1 exhibits Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS) and inhibits the growth of melanoma cells [1]. (In the molecular structure, target protein ligand: BI-882370 (HY-107779), red part; E3 ubiquitin enzyme ligand: Pomalidomide (HY-10984), blue part; PROTAC linker: G007-LK (HY-12438), black part.
|
-
- HY-131183
-
|
|
PROTACs
PD-1/PD-L1
|
Inflammation/Immunology
|
|
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner [1].
|
-
- HY-146393
-
|
|
PROTACs
Cytochrome P450
|
Cancer
|
|
PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer [1].
|
-
- HY-158551
-
|
|
PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC BcI-2/BcI-xI Degrader-1 (15) is a PROTAC based BcI-2/BcI-xI degrader (Red: BcI-2/BcI-xI inhibitor (HY-158677), black: linker, Blue: E3 ligase ligand) [1].
|
-
- HY-125876
-
|
|
PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 [1] (Blue: CRBN ligand, Black: linker；Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).
|
-
- HY-169151
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4-DCAF1 degrader-1 (I-907) is a BRD4-DCAF1 PROTAC degrader, DC50 is 10~100 nM. (Pink: BRD4-DCAF1 ligand (HY-169152); Black: linker (HY-126976); Blue: E3 ligase ligand (HY-15846)) [1].
|
-
- HY-125878
-
|
SGK3-PROTAC1
|
PROTACs
SGK
|
Cancer
|
|
PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a von Hippel-Lindau ligand-based SKG3 PROTAC composed of a PEG3-C4-OBn (HY-130620) alkyl linker, an SGK3 degrader (red structure), and a VHL ligand (HY-150803, blue structure). PROTAC SGK3 degrader-1 (0.3 μM) induced 50% endogenous SGK3 degradation within 2 hours, and 80% SGK3 degradation was observed at 8 hours, accompanied by loss of phosphorylation of NDRG1 (SGK3 substrate) [1].
|
-
- HY-168190
-
|
|
PROTACs
|
Cancer
|
|
PROTAC TBL1X degrader-1 (Compound TD11) is a PROTAC degrader for Transducin β-like protein 1 X-linked (TBL1X), and exhibits cytotoxicity in lymphoma cell Riva, Pfeiffer and Granta-519 with IC50 of 0.795, 0.397 and 0.522 μM, respectively. (Pink: ligand for target protein: TBL1X ligand 1 (HY-168191); Black: linker (HY-168193); Blue: ligand for E3 ligase: Thalidomide 4-fluoride (HY-41547)) [1]
|
-
- HY-162665
-
|
|
Histone Methyltransferase
|
Others
|
|
WIZ degrader 1 (Compound 141) is a degrader for widely interspaced zinc finger motifs (WIZ) with an AC50 of 2 nM. WIZ degrader 1 induces the expression of fetal hemoglobin (HbF) with an EC50 of 6 mM. WIZ degrader 1 is used in research of inherited blood disorders [1].
|
-
- HY-155582
-
|
|
Src
|
Cancer
|
|
BLK degrader 1 (compound 9) is a selective degrader of B-lymphoid tyrosine kinase (BLK). BLK degrader 1 shows anticancer activity in several B-lymphoid cell lines [1].
|
-
- HY-176421
-
|
|
PROTACs
PI3K
|
Cancer
|
|
PROTAC PI3K/110β degrader-1 (J-9) is a PROTAC based PI3K/110β degrader (Red: PI3K/110β inhibitor (HY-75124), black: linker, Blue: E3 ligase ligand) [1].
|
-
- HY-142925
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 1 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 1 has the potential for the research of cancer diseases (extracted from patent WO2021139756A1, compound 11) [1].
|
-
- HY-144624
-
|
|
PROTACs
TAM Receptor
|
Cancer
|
|
PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 μM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis [1].
|
-
- HY-162318
-
|
|
Molecular Glues
c-Myc
|
Cancer
|
|
MYC degrader 1 (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors [1].
|
-
- HY-141482
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects [1].
|
-
- HY-174138
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NF-κB degrader 1 (Compound MD-1) is a NF-κB1 p105 subunit degrader. NF-κB degrader 1 shows anti-inflammatory activity (IC50 for inhibiting TNF-α is 2.02 μM, and for inhibiting NO is 5.40 μM). NF-κB degrader 1 induces p105 degradation dependent on the Cullin-RING ligase (CRL) SCFBTCP, suppressing NF-κB transcriptional activity. NF-κB degrader 1 is promising for research of inflammation-related diseases [1].
|
-
- HY-162960
-
|
|
Ras
|
Cancer
|
|
pan-KRAS degrader 1 (Compound 1) is a panKRAS degrader with a surface plasmon resonance (SPR) dissociation constant Ki value of 25 nM for KRAS G12V .pan-KRAS degrader 1 has antitumor activity [1].
|
-
- HY-168654
-
|
|
Wee1
|
Cancer
|
|
WEE1 degrader 1 (Compound 10) is a Wee1 degrader with a DC50 value of 1.5 nM against Wee1. WEE1 degrader 1 possesses anti-cancer cell proliferation effects [1].
|
-
- HY-157458
-
|
|
ATTECs
Phosphodiesterase (PDE)
Autophagy
|
Cancer
|
|
PDEδ autophagic degrader 1 (compound 12c), an autophagosome-tethering compound (ATTEC). is a potent PDEδ autophagic degrader. PDEδ autophagic degrader 1 reduces the PDEδ protein level through lysosome-mediated autophagy without affecting the PDEδ mRNA expression. PDEδ autophagic degrader 1 suppresses the growth in KRAS mutant pancreatic cancer cells [1].
|
-
- HY-151606
-
|
|
Akt
|
Cancer
|
|
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer [1].
|
-
- HY-161324
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth [1].
|
-
- HY-162896
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
And1 degrader 1 (Compound A15) is a degrader of the acidic nucleoplasmic DNA-binding protein 1 (And1), which can significantly induce the degradation of And1 in NSCLC cells. And1 degrader 1 (5 μM) combined with Olaparib (HY-10162) (1 μM) effectively inhibits the proliferation of A549 and H460 cells. And1 degrader 1 can be used in cancer research [1].
|
-
- HY-119932
-
|
|
PROTACs
FAK
Akt
|
Cancer
|
|
PROTAC FAK degrader 1 (Compound PROTAC-3) is a selective and effective degrader of Fak PROTAC with a DC50 of 3.0 nM. PROTAC FAK degrader 1 reduces the ability of cancer cells to migrate and invade. PROTAC FAK degrader 1 can be used in the study of tumor. (Pink: Fak ligand (HY-44146); Black: Linker (HY-44141); Blue: VHL ligand 1 (HY-125845)) [1].
|
-
- HY-162307
-
|
|
PROTACs
Keap1-Nrf2
|
Cancer
|
|
Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with anticancer effects. Nrf2 degrader 1 inhibits cancer cells growth for A549 and LK-2 cells with IC50 values of 100 nM and 40 nM, respectively [1].
|
-
- HY-163814
-
|
|
PROTACs
CDK
|
Cancer
|
|
CDK2 degrader 1 (Compound 3) is an orally active cyclin-dependent kinase 2 (CDK2) degrader based on PROTAC technology. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers (Red: spiro[3.3]heptan-2- ylmethyl carbonochloridate; Blue: N,N-diisopropylethylamine; Black: linker) [1].
|
-
- HY-161101
-
|
|
PROTACs
IKZF Family
|
Cancer
|
|
MG degrader 1 (Compd E14) is a PROTAC degrader of IKZF3, GSPT1, and GSPT2 with an EC50 value of 1.385 nM in MM.1S cells [1].
|
-
- HY-169077
-
|
|
Molecular Glues
IKZF Family
|
Cancer
|
|
IKZF3 degrader 1 (compound 19a) is a molecular glue degrader of IKZF3 (EC50=0.012 μM). IKZF3 degrader 1 promotes the binding of IKZF3 to Cereblon (CRBN), leading to the ubiquitination and degradation of IKZF3 [1].
|
-
- HY-168950
-
|
|
Annexin A
|
Cancer
|
|
ANXA3 degrader 1 (Compound 18a5) is a highly selective ANXA3 degrader with cancer cell inhibition activity. ANXA3 degrader 1 displays excellent inhibitory effect in a triple-negative breast cancer (TNBC) tumor xenograft model (TGI=96%) [1].
|
-
- HY-161168
-
|
|
CDK
|
Cancer
|
|
Cyclin K degrader 1 (compound 40) is an AT7519 (HY-50940) based Cyclin K degrader with DC50 of 21 nM. Cyclin K degrader 1 has an affinity for cyclin K that is ~500-fold higher than its affinity for CDK12 [1].
|
-
- HY-149917
-
|
|
PROTACs
Itk
|
Cancer
|
|
ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice), with good plasma exposure levels. ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 consists of target protein ligand (red part) ITK ligand 1 (HY-168387), PROTAC linker (black part) Piperidine-C2-piperazine-Boc (HY-168388) and E3 ubiquitinase ligand (blue part) Thalidomide 5-fluoride (HY-W087383). E3 ubiquitinase and PROTAC linker can form Thalidomide-piperidine-C2-piperazine-Boc (HY-168389) [1].
|
-
- HY-130245
-
|
|
PCSK9
|
Metabolic Disease
|
|
PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor [1].
|
-
- HY-163640
-
-
- HY-162318A
-
|
|
Molecular Glues
c-Myc
|
Cancer
|
|
MYC degrader 1 TFA (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 TFA restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors [1].
|
-
- HY-146384
-
|
|
CRM1
|
Cancer
|
|
CRM1 degrader 1 (1l) is a low toxic chromosome region maintenance 1 (CRM1) degrader. CRM1 is the sole nuclear exporter of several tumor suppressor, a growth regulatory protein as an attractive cancer agent target. CRM1 degrader 1 induces the apoptosis in gastric carcinoma and selectively inhibits proliferation of gastric cancer [1].
|
-
- HY-169343
-
|
|
Molecular Glues
|
Cancer
|
|
FIZ1 degrader 1 (compound 1) is an IMiD-based molecular glue degrader targeting FIZ1 [1].
|
-
- HY-169235
-
-
- HY-162723
-
|
|
PROTACs
AP-1
|
Cancer
|
|
FOSL1 degrader 1 (4) is a T-5224-PROTAC, potently degrade FOSL1 (AP-1) to suppress cancer stemness gene expression in HNSCC. FOSL1 degrader 1 (4) effectively eliminate HNSCC cancer stem cells to inhibit tumor growth through degrading FOSL1. FOSL1 degrader 1 (4) displays around 30- to 100-fold increased potency over T-5224 (Pink: T-5224 (HY-12270); Black: Linker (HY-130200); Blue: Pomalidomide (HY-10984)) [1].
|
-
- HY-159728
-
|
|
Histone Methyltransferase
PROTACs
|
Cancer
|
|
PROTAC PRMT3 degrader 1 (compound 11) is a PROTAC degrader targeting PRMT3. PROTAC PRMT3 degrader 1 can inhibit the growth of acute leukemia cells [1].
|
-
- HY-162608
-
|
|
PROTACs
|
Cancer
|
|
PROTAC JAK1 degrader 1 degrader 1 (compound 10c) is an effective and selective PROTAC JAK1 degrader with a DC50 of 214 nM. PROTAC JAK1 degrader 1 has antitumor activity. (Structure Note: PINK, JAK1 ligand 1 (HY-10961); Blue, VHL ligand Thalidomide (HY-14658); Black, linker) [1].
|
-
- HY-162930
-
|
|
PROTACs
METTL3
|
Cancer
|
|
PROTAC METTL3 degrader 1 (Compound KH12) is a VHL-based PROTAC METTL3 degrader (DC50: 220 nM in MOLM-13 cells). PROTAC METTL3 degrader 1 inhibits METTL3/14 complex with an IC50 value of 341 nM. PROTAC METTL3 degrader 1 has anti-proliferative activities against AML cells. Black: Linker (HY-ER002); Red: METTL3 ligand (HY-115717); Blue: VHL ligand (HY-120217) [1].
|
-
- HY-130245A
-
|
|
PCSK9
|
Metabolic Disease
|
|
(R,R)-PCSK9 degrader 1 is the isomer of PCSK9 degrader 1 (HY-130245). PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor [1].
|
-
- HY-173467
-
|
|
PROTACs
c-Myc
|
Cancer
|
|
PROTAC MTP3 degrade-1 is a PROTAC based MYC degrader (Red: MYC inhibitor (HY-173469), black: linker (HY-W008296), Blue: E3 ligase ligand (HY-14658)) [1].
|
-
- HY-114323
-
|
|
PROTACs
FLT3
Apoptosis
STAT
MEK
ERK
|
Cancer
|
|
PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC50 of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor. (Pink: FLT3 ligand (HY-168702); Black: Linker (HY-124380); Blue: VHL ligand (HY-125845)) [1].
|
-
- HY-146368
-
|
|
PROTACs
VEGFR
|
Cancer
|
|
PROTAC VEGFR-2 degrader-1（PROTAC-1）, a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100 μM) [1].
|
-
- HY-163985
-
|
|
PROTACs
FGFR
Apoptosis
|
Cancer
|
|
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2.
PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM.
PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) [1].
|
-
- HY-152263
-
|
|
PROTACs
CDK
Apoptosis
|
Cancer
|
|
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer [1]. HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-169370
-
-
- HY-162626
-
|
|
PROTACs
FGFR
|
Cancer
|
|
FGFR2 degrader 1 (compound 28E) is a selectively PROTACS degrader of FGFR2, with the DC50 of 0.645 nM. FGFR2 plays an important role in cancer research (Pink: ligand of target protein; (HY-13304) black: linker; blue: ligand of E3 ligase) [1].
|
-
- HY-111758
-
|
|
PROTACs
Raf
|
Cancer
|
|
PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity [1].
|
-
- HY-111594
-
|
|
PROTACs
|
Cancer
|
|
Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3 [1].
|
-
- HY-168540
-
|
|
PROTACs
Mps1
Aurora Kinase
|
Cancer
|
|
PROTAC MPS1 degrader 1 (Compound 19) is a potent degrader of monopolar spindle 1 (Mps1, TTK), AURKA and AURKB, with DC50s of 17.7, 108.7 and 570.3 nM, respectively. PROTAC MPS1 degrader 1 can be used for the research of acute myeloid leukemia. (Pink: ligand for target protein (HY-168542); Black: linker (HY-W141926); Blue: ligand for E3 ligase (HY-10984) [1].
|
-
- HY-168896
-
|
|
CDK
ATTECs
|
Cancer
|
|
CDK9 autophagic degrader 1 (Compound 28) is a ATTEC degrader that can be used to degrade CDK9 and also affects the levels of the associated Cyclin T1. CDK9 autophagic degrader 1 shows over 80% CDK9 inhibition rate at 100 nM [1]. ( Pink: LC3B ligand (HY-168897); Black: linker (HY-W017758); Blue: target protein ligand (HY-10008); linker + target protein ligand (HY-168898))
|
-
- HY-155113
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC Hsp90α degrader 1 (Compound X10g) is a selective PROTAC Hsp90α degrader. PROTAC Hsp90α degrader 1 can be used for breast cancer research. PROTAC Hsp90α degrader 1 inhibits the proliferation of MDA-MB-231, MDA-MB-468, MCF-7, MX-1 cells with IC50s of 51.48 μM, 16.46 μM, 8.93 μM, 11.95 μM respectively [1].
|
-
- HY-168487
-
|
|
DNA/RNA Synthesis
PROTACs
WDR5
|
Others
|
|
PROTAC WDR5 degrader 1 (compound 8g) is a PROTAC degrader targeting WDR5. PROTAC WDR5 degrader 1 is composed of a target protein ligand (red part) WDR5 ligand 2 (HY-168488), a VHL-type E3 ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and a PROTAC linker (balck part) 5-Aminovaleric acid (HY-W015878), in which the VHL ligand and the PROTAC linker form a conjugate (HY-114176A) [1].
|
-
- HY-161597
-
|
|
PROTACs
|
Cancer
|
|
PROTAC DYRK2 degrader 1 (compound CP134) is a PROTAC degrader of DYRK2 (Red: DYRK2 inhibitor(HY-161598), black: linker (HY-42776), Blue: E3 ligase ligand (HY-10984)) [1].
|
-
- HY-162327
-
|
|
PROTACs
HBV
|
Infection
|
|
PROTAC PAPD5 degrader 1 (compound 12b) inhibits both hepatitis A (HAV) and hepatitis B virus (HBV) in vitro and in vivo [1], with IC50 and CC50 of 10.59 μM and ＞ 50 μM, respectively in Huh7 cells [1].
|
-
- HY-111593
-
|
|
PROTACs
|
Cancer
|
|
Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC [1], consists of two ligands of von Hippel-Lindau.
|
-
- HY-162282
-
|
|
PROTACs
DNA Methyltransferase
|
Cancer
|
|
PROTAC METTL3-14 degrader 1 (compound 30) is a PROTAC degrader of METTL3-14. PROTAC METTL3-14 degrader 1 shows a 50% or higher degradation of METTL3 and/or METTL14(Pink: Ligand for target protein (HY-115717); Black: Linker (HY-168686); Blue: Ligand for E3 ligase (HY-10984)) [1].
|
-
- HY-161176
-
|
|
PROTACs
|
Cancer
|
|
PROTAC KRAS G12D degrader 1 (compound 8o) is a potent, rapid, and selective degrader of protac KRAS G12D with DC 50 of 38.06 nM. PROTAC KRAS G12D degrader 1 showes significant antitumor efficacy [1].
|
-
- HY-163786
-
|
|
PROTACs
CDK
Apoptosis
|
Cancer
|
|
PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM. PROTAC CDK4/6 degrader 1 inhibits the proliferation of cell Jurkat (IC50 is 0.18 μM), arrests the cell cycle at G1 phase and induces apoptosis. (Pink: ligand for target protein YY173 (HY-163787); Black: linker (HY-163788); Blue: ligand for E3 ligase (HY-10984)) [1]
|
-
- HY-158381
-
|
|
PROTACs
Phosphatase
|
Metabolic Disease
|
|
PROTAC PTP1B degrader 1 (compound 75) is a CRBN-based PTP1B PROTAC degrader, with DC50 values of 0.2 μM (48 h) and 0.05 μM (72 h) (Red: PTP1B ligand Oleanolic acid (HY-N0156); Black: linker; Blue: CRBN ligand) [1].
|
-
- HY-159651
-
|
|
PROTACs
17β-HSD
|
Cancer
|
|
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] .
|
-
- HY-169134
-
|
|
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC 20S proteasome subunit β5 degrader 1 (compound 12f) is a targeted degrader of PROTAC for 20S proteasome subunit β5, with a DC50 value of 0.11 μM in FaDu cells. PROTAC 20S proteasome subunit β5 degrader 1 disrupts the cell cycle, promotes apoptosis, and inhibits cell proliferation and migration in both FaDu and KM3/BTZ cells. PROTAC 20S proteasome subunit β5 degrader 1 can be used to study the resistance of pharyngeal cancer and multiple myeloma to Bortezomib (HY-10227) (Pink: Target protein ligand (HY-10227); Blue: E3 ligase ligand (HY-103596); Black: Linker (HY-169142)) [1].
|
-
- HY-149434
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively [1].
|
-
- HY-152133
-
|
|
PROTACs
HDAC
Apoptosis
|
Cancer
|
|
PROTAC HDAC6 degrader (Compound A6) is a potent and selective PROTAC HDAC6 degrader with a DC50 of 3.5 nM. PROTAC HDAC6 degrader shows promising antiproliferative activity via inducing apoptosis in myeloid leukemia cell lines [1].
|
-
- HY-176476
-
-
- HY-21999
-
|
Tert-butyl 6-aminohexanoate
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 6-aminocaproate (Tert-butyl 6-aminohexanoate) is a PROTAC linker. tert-Butyl 6-aminocaproate can be used in synthesis PROTAC CARM1/IKZF3 degrader-1 (HY-172368) [1].
|
-
- HY-169152
-
-
- HY-168695
-
-
- HY-172828
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
BRD4 ligand 6 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). BRD4 ligand 6 can be used for synthesis PROTAC CBP/BRD4 degrader-1 (HY-172827) [1].
|
-
- HY-168318
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Bestatin-amide-PEG3-CH2-acid is an E3 ligase ligand-linker conjugate. Bestatin-amide-PEG3-CH2-acid can be used to synthesize PROTAC RAR Degrader-1 (HY-111844) [1].
|
-
- HY-131386A
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1?(HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM [1].
|
-
- HY-129776
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 2 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 2 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells [1].
|
-
- HY-129775
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells [1].
|
-
- HY-130991
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells [1].
|
-
- HY-156083
-
|
|
CDK
|
Cancer
|
|
PROTAC CDK9/CycT1 Degrader-1 (compounds 10) is a potent inhibitor of CDK9. PROTAC CDK9/CycT1 Degrader-1 can be used as a PROTAC target protein ligand for PROTAC synthesis. PROTAC CDK9/CycT1 Degrader-1 shows strong anti-proliferative activity in solid tumors [1].
|
-
- HY-145615
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C12-NH2 hydrochloride is the E3 ligase ligand-linker conjugate of PROTAC KRAS G12C degrader-1 (HY-139186). PROTAC KRAS G12C degrader-1 is a Cereblon-based KRAS G12C degrader .
|
-
- HY-160531
-
|
|
Molecular Glues
IKZF Family
|
Cancer
|
|
IKZF1-degrader-1 (Compound 9-B) is a IKZF1 molecular glue degrader with the DC50 value of 0.134 nM. IKZF1-degrader-1 can be used to degrader tumors [1].
|
-
- 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 [1].
|
-
- HY-130499
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα), and a PROTAC linker, which recruit E3 ligases MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader .
|
-
- HY-148837
-
|
|
PROTACs
c-Myc
Casein Kinase
|
Infection
Cardiovascular Disease
Cancer
|
|
PROTAC c-Myc degrader-1 (Compound A153) is a multiple target protein degrader (PROTAC). PROTAC c-Myc degrader-1 effective degrades c-MYC, CK1α, GSPT1 and IKZF1/2/3 proteins in a variety of tumor cells. PROTAC c-Myc degrader-1 can be used for c-Myc high expression related disease research, such as cancer, cardiovascular and cerebrovascular diseases, and viral infection (Pink: c-Myc ligand (HY-168685); Blue: E3 ligase ligand (HY-W093472); Black: linker (HY-W015808)) [1].
|
-
- HY-130620
-
|
|
PROTAC Linkers
|
Cancer
|
|
PEG3-C4-OBn is a polyethylene glycol (PEG)-based PROTAC linker. PEG3-C4-OBn can be used in the synthesis of the PROTAC SGK3 degrader-1 (HY-125878). PROTAC SGK3 degrader-1 is a potent SKG3 degrader based on PROTAC [1] .
|
-
- HY-168276
-
|
|
PROTAC Linkers
|
Cancer
|
|
Boc-Nonanol is a PROTAC linker. Boc-Nonanol can be used in the synthesis of PROTAC TRIB2 degrader-1 (HY-168274) [1].
|
-
- HY-W007587
-
|
|
PROTAC Linkers
|
Cancer
|
|
9-Bromononanoic acid is a PROTAC linker. 9-Bromononanoic acid can be used in synthesis PROTAC FGFR1 degrader-1 (HY-170869) [1].
|
-
- HY-158400
-
-
- HY-W411604
-
|
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl hex-5-ynoate is the linker that can be used for PROTAC synthesis of PROTAC cGAS degrader-1 (HY-172208) [1].
|
-
- HY-W013381
-
|
Decanoic acid, 10-bromo-
|
PROTAC Linkers
|
Others
|
|
10-Bromodecanoic acid (Decanoic acid, 10-bromo-) is a linker that can be used in the synthesis of PROTACs, such as PROTAC KDM4 degrader-1 (HY-173135) [1].
|
-
- HY-129968
-
|
|
PROTAC Linkers
|
Cancer
|
|
AM-Imidazole-PA-Boc is an alkyl chain-based PROTAC linker can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966) [1].
|
-
- HY-168191
-
-
- HY-163959
-
|
|
Lipase
|
Metabolic Disease
Cancer
|
|
PF-07853578 (Example 11) is a PNPLA3 degrader with an EC50 of 8 nM. PNPLA3 degrader-1 can be used in the study of cirrhosis and hepatocellular carcinoma [1].
|
-
- HY-176186
-
|
|
PROTAC Linkers
|
Cancer
|
|
4-Hydroxy-1-piperidinepropanamide is a PROTAC linker that can be used in the synthesis of PROTAC DDR1 degrader-1 (HY-176184) [1].
|
-
- HY-W584512
-
-
- HY-130819
-
|
|
PROTAC Linkers
|
Cancer
|
|
Tos-PEG4-THP is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523) [1].
|
-
- HY-W041652
-
|
|
ADC Linker
|
Cancer
|
|
5-Hydroxypentanoic acid is a PROTAC linker. 5-Hydroxypentanoic acid can be used in the synthesis of PROTAC AR-V7 degrader-1 (HY-145479) [1].
|
-
- HY-130814
-
|
|
E3 Ligase Ligand-Linker Conjugates
Autophagy
Apoptosis
|
Cancer
|
|
Thalidomide-NH-C4-NH2 TFA (compound 29c) is an E3 ligase ligand-linker conjugate, and incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-NH-C4-NH2 TFA is used in PROTAC BRD2/BRD4 degrader-1 (HY-130612). PROTAC BRD2/BRD4 degrader-1 is a potent and selective BET protein BRD4 and BRD2 degrader .
|
-
- HY-168193
-
|
|
PROTAC Linkers
|
Cancer
|
|
5-Amino-N-(3-bromopropyl)pentanamide is a PROTAC linker used in the synthesis of PROTAC TBL1X degrader-1 (HY-168190) [1].
|
-
- HY-W442085
-
|
|
PROTAC Linkers
|
Cancer
|
|
1,4-Di(3-hydroxypropoxy)butane is the linker of PROTAC Aster-A degrader-1 (HY-D233) and can be used for the synthesis of PROTAC [1].
|
-
- HY-130621
-
|
|
PROTAC Linkers
|
Cancer
|
|
OTs-C6-OBn is an alkyl chain-based PROTAC linker can be used in the synthesis of PROTAC SGK3 degrader-1 (HY-125878) [1].
|
-
- HY-168017
-
-
- HY-176490
-
-
- HY-176187
-
-
- HY-130852
-
-
- HY-168243
-
-
- HY-172218
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
Lenalidomide-hex-5-ynoic acid is a conjugate of E3 ligase ligand and linker, and can be used to synthesize PROTACs, such as PROTAC cGAS degrader-1 (HY-172208) [1].
|
-
- HY-176491
-
|
|
PROTAC Linkers
|
|
|
Alkyne-pyrazine-O-piperidine-(1-methylcyclopropyl) methanol is a PROTAC linker that can be used in the synthesis of PROTACs, such as PROTAC pan-KRAS degrader-1 (HY-176489) [1].
|
-
- HY-173137
-
-
- HY-176429
-
-
- HY-170672
-
-
- HY-W539427
-
-
- HY-168277
-
-
- HY-138678B
-
-
- HY-158678
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 27 (part of 15) is a ligand for E3 ligase, used for the synthesis of PROTAC BcI-2/BcI-xI Degrader-1 (HY-158551) [1]
|
-
- HY-30105
-
|
|
PROTAC Linkers
|
Cancer
|
|
N-Boc-piperazine is a Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183) [1].
|
-
- HY-W087383
-
|
|
Ligands for E3 Ligase
Autophagy
Apoptosis
|
Cancer
|
|
Thalidomide 5-fluoride is a thalidomide-based Cereblon ligand used to recruit Cereblon protein. Thalidomide 5-fluoride can be linked to target protein ligands (e.g. IRAK4) through a linker to form PROTAC molecules (e.g. PROTAC IRAK4 degrader-1). PROTAC IRAK4 degrader-1 caused <20%, >20-50%, and >50% IRAK4 protein degradation in OCI-LY-10 cells at concentrations of 0.01, 0.1, and 1 μM, respectively [1] .
|
-
- HY-173370
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
MAGL Ligand-Linker Conjugate 1 is a conjugate of the MAGL ligand and the linker. MAGL Ligand-Linker Conjugate 1 can be used for synthesis of PROTAC degrader PROTAC MAGL degrader-1 (HY-173369) [1].
|
-
- HY-168018
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Demethyl-NSC682769 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). Demethyl-NSC682769 can be used in synthesis PROTAC YAP degrader-1 (HY-168016) [1].
|
-
- HY-158679
-
-
- HY-168245
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 126 is an E3 Ligase Ligand-linker Conjugate, and can be used for synthesis of PROTACs, such as PROTAC BRM/BRG1 degrader-1 (HY-168242) [1].
|
-
- HY-176185
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
DDR1 ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). DDR1 ligand 1 can be used for the synthesis of PROTAC DDR1 degrader-1 (HY-176184) [1].
|
-
- HY-130816
-
|
VH032-O-Ph-PEG1-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02 [1].
|
-
- HY-W004701
-
|
|
PROTAC Linkers
|
Cancer
|
|
Br-C3-methyl ester is a Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183) [1].
|
-
- HY-130821
-
|
|
PROTAC Linkers
|
Cancer
|
|
THP-PEG4-Pyrrolidine(N-Me)-CH2OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523) [1].
|
-
- HY-130820
-
|
|
PROTAC Linkers
|
Cancer
|
|
THP-PEG4-Pyrrolidine(N-Boc)-CH2OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523) [1].
|
-
- HY-168275
-
-
- HY-170671
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 49 serves as the E3 ubiquitin ligase ligand for PROTAC XPO1 degrader-1 (HY-170669). E3 ligase Ligand 49 can be utilized for the synthesis of PROTACs [1].
|
-
- HY-159494
-
|
|
PROTACs
Epoxide Hydrolase
|
Metabolic Disease
|
|
sEH-degrader-1 (Compound 8) serves as an inhibitor for sEH, with IC50 values of 3.8 nM and 210 nM against hsEH and msEH respectively. sEH-degrader-1 can effectively degrade sEH in mouse liver and brown adipose tissue (Red: UC-1728 (HY-114266), black: linker (HY-W248248), Blue: Thalidomide-5-piperazine (HY-W834174)) [1].
|
-
- HY-32717
-
|
6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-ethoxyquinoline-3-carbonitrile
|
Ligands for Target Protein for PROTAC
|
Infection
|
|
DH03 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). DH03 can serve as an active control for the target protein ligand of PROTAC SARS-CoV-2 Degrader-1 (HY-174233) [1].
|
-
- HY-168039
-
|
|
PROTAC Linkers
|
Cancer
|
|
Boc-NH-Piperidine-C5-OH is a PROTAC linker. Boc-NH-Piperidine-C5-OH can be used in the synthesis of PROTAC PIN1 degrader-1 (HY-168037) [1].
|
-
- HY-168038
-
-
- HY-159619
-
|
|
PROTAC Linkers
|
Cancer
|
|
Boc-azetidine-2C-oxotetrahydropyrimidin-bromophenyl is a PROTAC Linker. Boc-azetidine-2C-oxotetrahydropyrimidin-bromophenyl can be used in the synthesis of PROTAC GSPT1 degrader-1 (HY-159609) [1].
|
-
- HY-131386
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
BMS-1166-N-piperidine-CO-N-piperazine incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM [1].
|
-
- HY-163852
-
-
- HY-158677
-
|
|
Bcl-2 Family
|
Cancer
|
|
BcI-2/BcI-xI ligand 1 is a BcI-2/BcI-xI ligand, and can be used for synthesis of PROTAC BcI-2/BcI-xI Degrader-1 (HY-158551) [1].
|
-
- HY-168192
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C4-amide-C3-Br is a conjugate of the E3 ligase ligand Thalidomide with a linker and can be used in the synthesis of PROTAC TBL1X degrader-1 (HY-168190) [1].
|
-
- HY-172370
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C4-Boc is the conjugate composed of an E3 ligase (Cereblon) ligand and a linker that can be used for synthesis of PROTAC CARM1/IKZF3 degrader-1 (HY-172368) [1].
|
-
- HY-172369
-
-
- HY-168244
-
|
|
PROTAC Linkers
|
Cancer
|
|
TsO-C2-Piperidine-O-azetidine-CO-Ph-C2-OH is a PROTAC linker, and can be used for PROTAC synthesis, such as PROTAC BRM/BRG1 degrader-1 (HY-168242) [1].
|
-
- HY-163960
-
|
|
PROTAC Linkers
|
Cancer
|
|
NH2-Ph-NH-cyclohexane-NH-Boc is a PROTAC linker. NH2-Ph-NH-cyclohexane-NH-Boc can be used in synthesis PROTAC erf3a Degrader-1 (HY-163938) [1].
|
-
- HY-170673
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 156 is a CRBN E3 ligase ligand-linker conjugate. E3 Ligase Ligand-linker Conjugate 156 can be used to synthesize PROTAC XPO1 degrader-1 (HY-170669) [1].
|
-
- HY-159452
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2/4-degrader-1 (compound I-430) 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 [1].
|
-
- HY-163864
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2 degrader-1 (compound I-321) is a PROTAC degrader of SMARCA with DC50＜100nM (red: SMARCA inhibitor, black: linker (HY-Y1215), blue: E3 ligase ligand (HY-163927) ) [1].
|
-
- HY-169371
-
|
|
SOS1
Drug Intermediate
|
Others
|
|
SOS1 Ligand intermediate-7 (65) is an intermediate for the synthesis of SOS1 ligand (HY-111671). SOS1 activator 1 (HY-111671) can be used for the synthesis of PROTAC SOS1 degrader-1 (HY-145737) [1].
|
-
- HY-174410
-
-
- HY-170996
-
|
|
ROR
|
Cancer
|
|
ROR1 ligand-1 (9-1) is a ligand for PROTACT ROR1 degrader-1 (HY-170995). ROR1 ligand-1 connects with VHL-type or CRBN ligand to design and synthesize the first selective and potent of ROR1 PROTACs [1].
|
-
- HY-129967
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
PROTAC IRAK4 ligand-1 is a synthetic ligand for interleukin-1 receptor-associated kinase 4 (IRAK4). PROTAC IRAK4 ligand-1 can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966) [1].
|
-
- HY-168040
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C5-piperidine-NH-Boc is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-O-C5-piperidine-NH-Boc can be used to synthesize PROTAC PIN1 degrader-1 (HY-168037) [1].
|
-
- HY-168643
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Me-(S,R,S)-AHPC-PEG2-OTs is a conjugate of E3 ligase ligand and linker (E3 Ligase Ligand-Linker Conjugates) used in the synthesis of PROTAC HIF-1α degrader-1 (HY-168641) [1].
|
-
- HY-131190
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
N-Boc-SBP-0636457-OH is a synthesized E3 ligase ligand-linker conjugate that incorporates IAP ligand and a linker. N-Boc-SBP-0636457-OH can be used to design a PROTAC Bcl-xL degrader-1 (HY-131188) [1].
|
-
- HY-W599025
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
5-Br-4-Cl-Pyrrolo-pyroxypyridine is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). 5-Br-4-Cl-Pyrrolo-pyroxypyridine can be used for synthesis PROTAC GSPT1 degrader-1 (HY-159609) [1].
|
-
- HY-176430
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-amide-pimelic acid is an E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based CRBN ligand and Linker (HY-Y1139). Lenalidomide-amide-pimelic acid can be used for synthesis of PROTAC MNK1 degrader-1 (HY-176428) [1].
|
-
- HY-159620
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide 5-azetidine-2C-oxotetrahydropyrimidin-bromophenyl is an E3 Ligase Ligand-Linker Conjugate. Thalidomide 5-azetidine-2C-oxotetrahydropyrimidin-bromophenyl can be used to synthesize PROTAC GSPT1 degrader-1 (HY-159609) [1].
|
-
- HY-131189
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
N-Boc-SBP-0636457-OH, a ligand for E3 ubiquitin ligase, is used in the recruitment of IAP E3 ligases. N-Boc-SBP-0636457-OH can be connected to the ligand for Bcl-xL by a linker to form PROTAC Bcl-xL degrader-1 (HY-131188).
|
-
- HY-41547
-
|
Cereblon ligand 4; E3 ligase Ligand 4
|
Ligands for E3 Ligase
Autophagy
Apoptosis
|
Cancer
|
|
Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966) [1].
|
-
- HY-159777
-
-
- HY-130813
-
-
- HY-131186
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amido-C3-piperazine-N-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183) [1].
|
-
- HY-176188
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-5-Br-amide-C2-Br is an E3 ligase ligand-linker conjugate. Lenalidomide-5-Br-amide-C2-Br can be used to synthesize PROTAC DDR1 degrader-1 (HY-176184) [1].
|
-
- HY-163904
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
(S,R,R)-VH032-CO-C3-CONH-C2-PEG3-OH is an E3 ligase ligand-linker conjugate of PROTAC NCOA4 degrader-1 (HY-163897), which can be used for the synthesis of PROTACs [1].
|
-
- HY-158343
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG2-C2-CH2 is a conjugate of E3 ligase ligand and linker. Thalidomide-NH-PEG2-C2-CH2 is utilized for synthesis of PROTAC TEAD degrader-1 (HY-158342) [1].
|
-
- HY-131184
-
|
|
PROTAC Linkers
|
Inflammation/Immunology
|
|
N-Boc-piperazine-C3-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-N-piperazine-C3-COOH can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183) [1].
|
-
- HY-168019
-
-
- HY-130713
-
-
- HY-176492
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 193 is an E3 ligase ligand-linker conjugate that incorporates the VHL Ligase Ligand (HY-170353) and linker (HY-176491). E3 Ligase Ligand-linker Conjugate 193 can be used for synthesis of PROTAC pan-KRAS degrader-1 (HY-176489) [1].
|
-
- HY-176422
-
-
- HY-163647
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-COCH-PEG2-azido is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based cereblon ligand and a linker. Lenalidomide-COCH-PEG2-azido can be used in the synthesis of PROTAC AKR1C3 degrader-1 (HY-163609) [1].
|
-
- HY-130712
-
|
|
PROTAC Linkers
|
Cancer
|
|
NH2-C2-amido-C2-Boc is a PROTAC linker, which refers to the alkyl/ether composition. NH2-C5-NH-Boc can be used in the synthesis of a series of PROTACs, such as the PROTAC CDK2/9 Degrader-1 (HY-130709) [1].
|
-
- HY-111671
-
|
SOS1 activator 1
|
SOS1
Ras
PERK
Ligands for Target Protein for PROTAC
|
Cancer
|
|
VUBI1 (SOS1 activator 1) is a benzimidazole derivative and SOS1 activator with a Kd of 44 nM. VUBI1 can significantly activate RAS-GTP and regulate the phosphorylation of ERK. VUBI1 also can serve as a target ligand for synthesizing PROTACs, such as PROTAC SOS1 degrader-1 (HY-145737), to induce SOS1 degradation. VUBI1 can be used in the study of cancer [1] .
|
-
- HY-150839
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand PG is a E3 ligase ligand that can be used in the recruitment of CRBN protein. E3 ligase Ligand PG exhibits potent binding activity with CRBN (IC50 of 2.191 μM). E3 ligase Ligand PG can be connected to the BMS-202 (HY-19745) by a linker to form PROTAC, PROTAC PD-L1 degrader-1 (HY-163757) [1].
|
-
- HY-130822
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 4 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 4 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells [1].
|
-
- HY-130823
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 5 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 5 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells [1].
|
-
- HY-130815A
-
-
- HY-130815
-
-
- HY-130707
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 3 (Compound 001371) incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells [1].
|
-
- HY-161709
-
|
|
Ligands for Target Protein for PROTAC
FLT3
CDK
|
Cancer
|
|
FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependent kinase (CDK) and the FMS-like tyrosine kinase 3 (FLT3), inhibits FLT3/CDK related proliferations and survivals of leukemia cells. LT3/CDKs ligand-1 can be used for synthesis of PROTAC FLT3/CDKs degrader-1 (HY-161708) [1].
|
-
- HY-174235
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Infection
|
|
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 SARS-CoV-2 Degrader-1 (HY-174233) [1].
|
-
- HY-130619
-
|
|
PROTAC Linkers
|
Cancer
|
|
Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins [1].
|
-
- HY-131187
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1 [1]. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation .
|
-
- HY-130984
-
|
|
PROTAC Linkers
|
Cancer
|
|
Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker. Azido-PEG1-CH2COO-Cl can be used in the synthesis of PROTAC BRD4 Degrader-1 (HY-133131) [1]. Azido-PEG1-CH2COO-Cl 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-168694
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 147 is a conjugate of E3 ligase ligand and PROTAC Linker, which can be used to synthesize BRD9 Degrader-1 (HY-156401) (Compound 13-7) [1]. E3 Ligase Ligand-linker Conjugate 147 is composed of the E3 ligase ligand BRD9 ligand-7 (HY-168695) and the PROTA linker 2-((1R,5S,6s)-3-Azabicyclo[3.1.0]hexan-6-yl)ethan-1-ol (HY-W763939).
|
-
- HY-133138
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker.?Pomalidomide-PEG1-azide?can be used to design a?PROTAC BRD4 Degrader-1 (HY-133131) [1]. Pomalidomide-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-108369
-
|
|
PROTAC Linkers
|
Cancer
|
|
Azido-PEG1-CH2CO2H is a PROTAC linker, which refers to the alkyl/ether composition. Azido-PEG1-CH2CO2H can be used in the synthesis of PROTAC BRD4 Degrader-1 [1]. Azido-PEG1-CH2CO2H 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-162098
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
PROTAC tubulin-IN-1 (compound W13) is an inhibitor of PROTAC tubulin. PROTAC tubulin-IN-1 exhibits antitumor activity against human lung cancer [1].
|
-
- HY-173469
-
|
|
c-Myc
|
Cancer
|
|
MTP3 ligand-1 is a MTP3 ligand for PROTAC MTP3 degrade-1 (HY-173467). PROTAC MTP3 degrade-1 is a PROTAC based MYC degrader .
|
-
- HY-142662
-
|
|
PROTACs
|
Others
|
|
PROTAC IRAK3 degrade-1 (compound 23) is a potent and selective degrader of IRAK3 (IC50 = 5 nM) [1].
|
-
- HY-142662A
-
|
|
PROTACs
|
Others
|
|
PROTAC IRAK3 degrade-1 (compound 23) formic is a potent and selective degrader of IRAK3 (IC50=5 nM) [1].
|
-
- HY-159592
-
|
|
PROTAC Linkers
|
Cancer
|
|
Piperazine-Pyrimidine-Cyclohexane-COOEt is a PROTAC linker. Piperazine-Pyrimidine-Cyclohexane-COOEt can be used in the synthesis of PROTAC SMARCA2/4-degrader-1 (HY-159452) [1].
|
-
- HY-137343
-
-
- HY-161796A
-
-
- HY-173470
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
MTP3 Ligand-linker Conjugate 1 is a conjugate of the MTP3 ligand and the linker. MTP3 Ligand-linker Conjugate 1 can be used for synthesis of PROTAC MTP3 degrade-1 (HY-173467) [1].
|
-
- HY-N8180
-
|
|
Others
|
Others
|
|
Silyamandin is a flavonolignan compound. Silydianin can form Silyamandin through oxidative degradation .
|
-
- HY-155398
-
-
- HY-155397
-
-
- HY-159593
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Ac-NH-(S,R,S)-AHPC-CO-cyclohexane-pyrimidine-diazabicyclo is an E3 Ligase Ligand-Linker Conjugate. Ac-NH-(S,R,S)-AHPC-CO-cyclohexane-pyrimidine-diazabicyclo can be used to synthesize PROTAC SMARCA2/4-degrader-1 (HY-159452) [1].
|
-
- HY-157582
-
|
|
EGFR
|
Others
|
|
MS39N (compound 27) is a negative control for MS39 that binds EGFR without inducing degradation .
|
-
- HY-158767
-
|
|
Drug Derivative
|
Others
|
|
Dehydro amlodipine fumarate is a derivative of Dehydro amlodipine and is one of the forced degradation products of Dehydro amlodipine during oxidation and acid degradation .
|
-
- HY-E70529
-
|
|
DNA/RNA Synthesis
|
Others
|
|
Ribonucleoside vanadyl complexes is a ribonuclease (RNase) inhibitor that can be used in RNA isolation and detection to inhibit RNA degradation .
|
-
- HY-150400
-
|
|
PROTACs
WDR5
|
Cancer
|
|
XF056-132 free base is a potent WDR5 (WD40 repeat domain protein 5) PROTAC degrader .
|
-
- HY-163989
-
|
|
PROTAC Linkers
|
Cancer
|
|
N-Ethylheptanamide is a PROTAC linker. N-Ethylheptanamide can be used in synthesis PROTAC FGFR2 degrader 1 (HY-163985) [1].
|
-
- HY-168488
-
-
- HY-153042
-
-
![Thalidomide-NH-C2-azaspiro[3.5]nonane hydrochloride](//file.medchemexpress.eu/product_pic/hy-153042.gif)
- HY-130617
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity [1].
|
-
- HY-N2057
-
|
|
Aquaporin
|
Metabolic Disease
|
|
Steviol is a major metabolite of the sweetening compound stevioside. Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation .
|
-
- HY-113136
-
|
N1-Methylguanosine
|
Endogenous Metabolite
|
Cancer
|
|
1-Methylguanosine (N1-Methylguanosine) is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker [1].
|
-
- HY-139340
-
|
|
PROTACs
|
Others
|
|
Photo-lenalidomide-acid (compound 3) is a photacts consist of a ligand for an E3 ligase, a photoswitch, and a ligand for a protein of interest and enable optical control of protein degradation .
|
-
- HY-NP200
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Keratin azure can be used to monitor the degradation of (β)-keratin. Keratin azure can be used as a substrate in keratin assays to assess keratinase degradation .
|
-
- HY-131230
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
Desmorpholinyl Quizartinib-PEG2-COOH incorporates a ligand for FLT-3, and a PEG-based PROTAC linker. Desmorpholinyl Quizartinib-PEG2-COOH can be used in the synthesis of PROTAC FLT-3 degrader 1 (HY-114323). PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM [1].
|
-
- HY-118653
-
|
|
MAGL
|
Metabolic Disease
|
|
SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation .
|
-
- HY-141551B
-
|
|
Drug Isomer
|
Others
|
|
(R)-GNE-274 is a enantiomer of GNE-274. GNE-274 is a non-degrader that is structurally related to GDC-0927 (estrogen receptor degrader) .
|
-
- HY-120722
-
TCH-165
1 Publications Verification
|
Proteasome
|
Cancer
|
|
TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation .
|
-
- HY-44146
-
-
- HY-130640
-
-
- HY-168897
-
-
- HY-114406
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation .
|
-
- HY-W017389
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
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-159733
-
-
- HY-161598
-
-
- HY-W248248
-
|
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 9-aminononanoate is a PROTAC linker. tert-Butyl 9-aminononanoate can be used in synthesis PROTAC sEH-degrader-1 (HY-159494) [1].
|
-
- HY-162973
-
-
- HY-169094
-
-
- HY-W749852
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Xanthine sodium, 98%, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine sodium, 98% also acts as an intermediate product on the pathway of purine degradation .
|
-
- HY-161575
-
-
- HY-145514A
-
|
|
PROTACs
FKBP
|
Cancer
|
|
dTAGV-1-NEG is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1 is an FKBP12 F36V-selective degrader .
|
-
- HY-135345
-
|
|
PROTACs
FKBP
|
Cancer
|
|
PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader .
|
-
- HY-W749852A
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Xanthine sodium, for cell culture, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine sodium, for cell culture also acts as an intermediate product on the pathway of purine degradation .
|
-
- HY-168898
-
-
- HY-168702
-
-
- HY-158767R
-
|
|
Drug Derivative
Reference Standards
|
Others
|
|
Dehydro amlodipine (fumarate) (Standard) is the analytical standard of Dehydro amlodipine (fumarate). This product is intended for research and analytical applications. Dehydro amlodipine fumarate is a derivative of Dehydro amlodipine and is one of the forced degradation products of Dehydro amlodipine during oxidation and acid degradation .
|
-
- HY-133799
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C7-COOH is a synthesized E3 ligase cereblon ligand-linker conjugate. Pomalidomide-C7-COOH is an intermediate for the synthesis of PROTAC BCL-XL degraders .
|
-
- HY-P2191
-
|
|
Kisspeptin Receptor
|
Endocrinology
|
|
KISS1-305, the Metastin/Kisspeptin analog, is a prototype peptide and a chemical probe. KISS1-305 has suboptimal KISS1R agonistic activity, and resists plasma protease degradation .
|
-
- HY-169158
-
-
- HY-168288
-
-
- HY-159660
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 31 is a ligand for E3 ubiquitinase. E3 ligase Ligand 31 can be used to synthesize PTOTAC HSD17B13 degrader 1 (HY-159651) [1].
|
-
- HY-160438A
-
|
|
Others
|
Cancer
|
|
PBX-7011 mesylate is an active Camptothecin (HY-16560) derivative. PBX-7011 can bind to the DDX5 protein in cells, thereby inducing cell death through DDX5 protein degradation .
|
-
- HY-W016087
-
|
|
PROTAC Linkers
|
Cancer
|
|
Monoethyl pimelate is a PROTAC linker, which refers to the alkyl/ether composition. Monoethyl pimelate can be used in the synthesis of (S,R,S)-AHPC-Me-C7 ester, a specific BCL-XL PROTAC degrader .
|
-
- HY-160438
-
|
|
Survivin
|
Cancer
|
|
PBX-7011 is an active camptothecin (HY-16560) derivative. PBX-7011 can bind to the DDX5 protein in cells, thereby inducing cell death through DDX5 protein degradation .
|
-
- HY-173599
-
|
|
Lipase
|
Cancer
|
|
NUV-244 is a PNPLA3 I148M degrader. NUV-244 reduces PNPLA3 I148M levels on lipid droplets via BFAR-mediated ubiquitin-proteasome degradation .
|
-
- HY-145514B
-
|
|
PROTACs
FKBP
|
Cancer
|
|
dTAGV-1-NEG TFA is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1-NEG TFA is an FKBP12 F36V-selective degrader .
|
-
- HY-130770
-
|
|
PROTAC Linkers
|
Cancer
|
|
Ald-CH2-PEG3-CH2-Boc is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of SGK3 kinase PROTAC degrader .
|
-
- HY-157592
-
-
- HY-113136R
-
|
|
Endogenous Metabolite
|
Cancer
|
|
1-Methylguanosine (Standard) is the analytical standard of 1-Methylguanosine. This product is intended for research and analytical applications. 1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker [1].
|
-
- HY-161746
-
|
|
AUTOTACs
Autophagy
|
Cancer
|
|
Anle138b-F105 is an autophagy targeting chimera (AUTOTAC) with DC50 values of 3 nM. Anle138b-F105 targetes tauP301L for lysosomal degradation .
|
-
- HY-N2057R
-
|
|
Reference Standards
Aquaporin
|
Metabolic Disease
|
|
Steviol (Standard) is the analytical standard of Steviol. This product is intended for research and analytical applications. Steviol is a major metabolite of the sweetening compound stevioside. Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation .
|
-
- HY-148523
-
|
|
Molecular Glues
CDK
|
Cancer
|
|
HQ005 is a potent CCNK degrader with an DC50 value of 0.041 µM. HQ005 is a molecular-glue degrader that mediates interactions between target proteins and components of the ubiquitin-proteasome system to cause selective protein degradation .
|
-
- HY-168687
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 137 is the linker and E3 ligase ligand for the PROTAC METTL3-14 degrader 1 (HY-162282), which can be used for research on acute myeloid leukemia [1].
|
-
- HY-169395
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-CO-PEG-C2-iodine is an E3 ligase (VHL) ligand-linker conjugate, and can be used for synthesis of PROTACs, such as PROTAC FAK degrader 1 (HY-119932) [1]
|
-
- HY-129363
-
-
- HY-124449
-
|
ME-5343
|
TRP Channel
|
Others
|
|
Afidopyropen (ME-5343) is an Afidopyropen targets sucking insects such as whiteflies, aphids, and leafhoppers by acting on the Nanchung (Nan) and Inactive (Iav) encoding gene of insects, and affecting TRPV channel. Afidopyropen can be used for many crops for its degradability .
|
-
- HY-D2259
-
|
|
E1/E2/E3 Enzyme
|
Others
|
|
PFI-7 is a probe, which binds to human GID4 (KD is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation .
|
-
- HY-44141
-
|
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 3-(2-iodoethoxy)propanoate is a PROTAC linker, which refers to the PEG composition. tert-Butyl 3-(2-iodoethoxy)propanoate can be used in the synthesis of PROTAC FAK degrader 1 (HY-119932) [1].
|
-
- HY-168686
-
|
|
PROTAC Linkers
|
Cancer
|
|
6-Hydroxy-1-(4-(2-hydroxyethyl) piperazin-1-yl) hexan-1-one is the linker for PROTAC METTL3-14 degrader 1 (HY-162282) [1].
|
-
- HY-156395
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
MN551 is a potent inhibitor of cysteine-directed electrophilic covalent that plays important roles in the biology of SOCS2 and its CRL5 complex, and as E3 ligase handles in proteolysis targeting chimera (PROTACs) to induce targeted protein degradation .
|
-
- HY-136183
-
|
VH032 phenol-alkylC6-amine dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-phenol-alkylC6-amine dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and an alkyl linker used for PROTAC degrader .
|
-
- HY-162610
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-alkyne-C4-NHBoc is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-alkyne-C4-NHBoc can be used to synthesize PROTAC JAK1 degrader 1 (HY-162608) [1].
|
-
- HY-128839
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
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 .
|
-
- HY-44148
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation .
|
-
- HY-126534A
-
|
LSN3106729 hydrochloride
|
Ligands for Target Protein for PROTAC
CDK
|
Cancer
|
|
Abemaciclib metabolite M18 (LSN3106729) hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
|
-
- HY-126534
-
-
- HY-130800
-
-
- HY-159661
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 114 is an E3 ubiquitinase ligand + linker conjugate. E3 Ligase Ligand-linker Conjugate 114 can be used to synthesize PTOTAC HSD17B13 degrader 1 (HY-159651) [1].
|
-
- 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) [1].
|
-
- HY-W003696
-
|
Tert-butyl 5-bromo-1,3-dihydro-2H-isoindole-2- carboxylate
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 5-bromoisoindoline-2-carboxylate is a PROTAC Linker. tert-Butyl 5-bromoisoindoline-2-carboxylate can be used in synthesis PTOTAC HSD17B13 degrader 1 (HY-159651) [1].
|
-
- HY-157591
-
-
- HY-130648
-
-
- HY-162411
-
|
|
Others
|
Cancer
|
|
E3 ligase Ligand 24 (Compound 24) is a Potent Ligand for the E3 Ligase DCAF15 (IC50= 0.053 μM). Due to E3 ligase Ligand 24’s selectivity and potent binding characteristics, it is pivotal in the study of targeted protein degradation .
|
-
- HY-163986
-
-
- HY-131717A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-CH2-COOH TFA is a ligand-linker conjugate for the E3 ligase Cereblon (CRBN). Thalidomide-NH-CH2-COOH TFA can be conjugated to multi-targeted kinase inhibitors to transform them into selective degraders .
|
-
- HY-13822
-
SKI II
5 Publications Verification
|
SphK
Wnt
Apoptosis
|
Cancer
|
|
SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation .
|
-
- HY-122702
-
|
|
PROTAC Linkers
|
Others
|
|
PEG6-(CH2CO2H)2 is a symmetric PEG PROTAC linker, for the synthesis of Homo-PROTACs which is bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation .
|
-
- HY-W998281
-
|
|
Drug Intermediate
|
Others
|
|
3-(4-(5-Hydroxypent-1-yn-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione (Compound 15c) is an important intermediate in the synthesis of RET Degrader .
|
-
- HY-137342
-
|
|
PROTACs
|
Cancer
|
|
SB1-G-187, a PROTAC, is a multi-kinase degrader . SB1-G-187 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-122725B
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-C5-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader .
|
-
- HY-144605
-
|
|
EGFR
PROTACs
|
Cancer
|
|
PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation .
|
-
- HY-122725A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader .
|
-
- HY-113136S
-
|
N1-Methylguanosine-d3
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Cancer
|
|
1-Methylguanosine-d3 (N1-Methylguanosine-d3) is deuterium labeled 1-Methylguanosine (HY-113136). 1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker [1] .
|
-
- HY-W457949
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Pomalidomide 4'-alkylC4-azide (Compound 2) is an azide compound containing a MIDI group and is one of the compounds used to construct a library of MIDI azide compounds. Pomalidomide 4'-alkylC4-azide can be used to develop research on PROTAC degraders .
|
-
- HY-132288
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader .
|
-
- HY-163787
-
|
|
CDK
|
Cancer
|
|
YY173 is a dual inhibitor for CDK4 and CDK6 with IC50 of 7.7 and 88 nM. YY173 inhibits the proliferation of cell Jurkat with an IC50 of 1.46 μM. YY173 can be used for synthesis of PROTAC CDK4/6 degrader 1 (HY-163786) [1].
|
-
- HY-W017389S
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
Xanthine- 13C, 15N2 is a 15N-labeled and 13C-labled Xanthine (HY-W017389). Xanthine is a plant alkaloid with mild stimulant activity of the central nervous system. Xanthine also acts as an intermediate product on the pathway of purine degradation .
|
-
- HY-170429
-
|
|
PIN1
|
Cancer
|
|
BJP-07-017-3 is the inhibitor for proline cis trans isomerase (Pin1) with an IC50 of 9 nM. BJP-07-017-3 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation .
|
-
- HY-13982
-
JSH-23
Maximum Cited Publications
107 Publications Verification
|
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation .
|
-
- HY-168055
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(S)-Deoxy-thalidomide is an E3 ubiquitin ligase ligand. (S)-Deoxy-thalidomide can be linked to the target protein ligand through a linker to form PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can target KRAS mutant proteins for degradation .
|
-
- HY-136186
-
|
VH032-C7-amine
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-158383
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-CO-C3-PEG4-C6-NH2 is an E3 ligase ligand-linker conjugate part of PROTAC PIPIB degrader 1 (HY-158381). Pomalidomide consists of the E3 ligase ligand Pomalidomide (HY-10984) and a linker [1].
|
-
- HY-136186B
-
|
VH032-C7-amine hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-131295
-
|
|
MEK
Ligands for Target Protein for PROTAC
|
Cancer
|
|
PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader .
|
-
- HY-136187
-
|
VH032-C5-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-136187A
-
|
VH032-C5-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-114407
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM [1]. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .
|
-
- HY-126534S
-
|
LSN3106729-d8
|
CDK
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
|
-
- HY-157765
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-6 (compound A2) is a potent PROTAC degrader of ERα, with IC50 of 0.11 μM in MCE-7 cells. PROTAC ERα Degrader-6 has anti-tumor effect. PROTAC ERα Degrader-6 is a fluorescent probes with Em of 582 nm that enable real-time visualization of ERα protein degradation .
|
-
- HY-168290
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide can be used in the synthesis of PROTACs, such as MS934 (HY-153863). MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader .
|
-
- HY-167701
-
|
|
Ligands for Target Protein for PROTAC
Apoptosis
Estrogen Receptor/ERR
|
Cancer
|
|
OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders .
|
-
- HY-W017389R
-
|
|
Reference Standards
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Xanthine (Standard) is the analytical standard of Xanthine. This product is intended for research and analytical applications. 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 .
In Vitro: A number of stimulants are derived from Xanthine including caffeine and theobromine. Xanthine is a product on the pathway of purine degradation. Xanthine is subsequently converted to uric acid by the action of the Xanthine oxidase enzyme.
|
-
- HY-13982R
-
|
|
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
JSH-23 (Standard) is the analytical standard of JSH-23. This product is intended for research and analytical applications. JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation .
|
-
- HY-N6769
-
|
Monorden
|
HSP
Bacterial
Antibiotic
Parasite
|
Infection
|
|
Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation . Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB . Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM .
|
-
- HY-111836
-
|
|
Molecular Glues
β-catenin
|
Cancer
|
|
NRX-252114 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF β-TrCP. NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. NRX-252114 induces mutant β-catenin degradation .
|
-
- HY-141894
-
|
|
Histone Acetyltransferase
|
Metabolic Disease
|
5-Ph-IAA-AM is an eggshell-permeable 5-Ph-IAA (HY-134653) analog which contains an acetoxymethyl (AM) group. 5-Ph-IAA-AM affords an enhanced protein degradation in laid embryos. 5-Ph-IAA-AM can be used to disclosure the roles of proteins in C. elegans, in particular those that are involved in embryogenesis and development, through temporally controlled protein degradation .
|
-
- 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) [1].
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- HY-133046
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader . VHL Ligand-Linker Conjugates 17 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-136186A
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VH032-C7-amine dihydrochloride
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C7-amine dihydrochloride is the dihydrochloride form of (S,R,S)-AHPC-C7-amine (HY-136186). (S,R,S)-AHPC-C7-amine is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker. (S,R,S)-AHPC-C7-amine can be used for estrogen-related receptor α (ERRα) PROTAC degrader .
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- HY-129619
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SNIPERs
Estrogen Receptor/ERR
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Cancer
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SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation .
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- HY-130711
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VH032-C3-NH2
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
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- HY-130711A
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VH032-C3-NH2 TFA
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C3-NH2 TFA (VH032-C3-NH2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
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- HY-159788
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PROTACs
Ras
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Cancer
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PROTAC K-Ras Degrader-4 (Compound 4) is a PROTAC degrader for KRAS that degrades KRAS G12D in GP5d and degrades KRAS G12V in cell SW620 with DC50s of 1 nM and 13 nM. PROTAC K-Ras Degrader-4 inhibits MAPK signaling pathway [1]. (Pink: ligand for target protein pan-KRAS degrader 1 (HY-162960); Black: linker (HY-159790); Blue: ligand for E3 ligase VHL (HY-W998248))
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- HY-145177
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc can be used for the synthesis of PROTAC BET degrader . (From patent WO2017180417A1 compound s7).
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- HY-144995
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CDK4/6-IN-11
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PROTACs
CDK
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Cancer
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CDK4/6-IN-11 is a potent PROTAC CDK4/6 degrader . CDK4/6-IN-11 consists of a thalidomide-based E3 ligase ligand (blue part) Thalidomide-NH-CH2-COOH (HY-131717), a target protein ligand (red part) Palbociclib (HY-50767), and a PROTAC linker (black part) Boc-NH-C4-Br (HY-W007803). E3 ligase ligand and linker can form Thalidomide-NH-amido-C4-Br (HY-170307).
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- HY-130711C
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VH032-C3-NH2 dihydrochloride
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C3-NH2 (dihydrochloride) is the dihydrochloride form of (S,R,S)-AHPC-C3-NH2 (HY-130711). (S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
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- HY-157228
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PROTACs
Ras
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Cancer
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ACBI3 (compound 7) is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models [1] .
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- HY-130652
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1?degrader based on Rucaparib by using the PROTAC approach [1]. Pomalidomide 4'-PEG3-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-151792
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E3 Ligase Ligand-Linker Conjugates
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Metabolic Disease
Inflammation/Immunology
Cancer
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Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. Pomalidomid-C6-PEG3-butyl-N3 also is a crosslinker-E3 ligase ligand conjugate, which be used in click reactive protein degrader building block for PROTAC research.
Pomalidomid-C6-PEG3-butyl-N3 also can be used in the template for synthesis of targeted protein degrader . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
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| Cat. No. |
Product Name |
Type |
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- HY-D2336
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Fluorescent Dyes/Probes
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PROTAC Aster-A degrader-1 (compound NGF3) is a degrader of the sterol transport protein Aster-A. PROTAC Aster-A degrader-1 can be used as a fluorescence probe. (Red: Aster-A inhibitor, black: linker, Blue: E3 ligase ligand) [1].
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- HY-D2259
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Fluorescent Dyes/Probes
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PFI-7 is a probe, which binds to human GID4 (KD is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation .
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| Cat. No. |
Product Name |
Type |
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- HY-NP200
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Enzyme Substrates
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Keratin azure can be used to monitor the degradation of (β)-keratin. Keratin azure can be used as a substrate in keratin assays to assess keratinase degradation .
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- HY-W749852
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Enzyme Substrates
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Xanthine sodium, 98%, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine sodium, 98% also acts as an intermediate product on the pathway of purine degradation .
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- HY-W749852A
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Enzyme Substrates
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Xanthine sodium, for cell culture, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine sodium, for cell culture also acts as an intermediate product on the pathway of purine degradation .
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| Cat. No. |
Product Name |
Target |
Research Area |
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-113136S
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1-Methylguanosine-d3 (N1-Methylguanosine-d3) is deuterium labeled 1-Methylguanosine (HY-113136). 1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker [1] .
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- HY-W017389S
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Xanthine- 13C, 15N2 is a 15N-labeled and 13C-labled Xanthine (HY-W017389). Xanthine is a plant alkaloid with mild stimulant activity of the central nervous system. Xanthine also acts as an intermediate product on the pathway of purine degradation .
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- HY-126534S
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Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
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| Cat. No. |
Product Name |
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Classification |
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- HY-133138
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PROTAC Synthesis
Azide
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Pomalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker.?Pomalidomide-PEG1-azide?can be used to design a?PROTAC BRD4 Degrader-1 (HY-133131) [1]. Pomalidomide-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-108369
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Azide
PROTAC Synthesis
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Azido-PEG1-CH2CO2H is a PROTAC linker, which refers to the alkyl/ether composition. Azido-PEG1-CH2CO2H can be used in the synthesis of PROTAC BRD4 Degrader-1 [1]. Azido-PEG1-CH2CO2H 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-130652
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Azide
PROTAC Synthesis
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Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1?degrader based on Rucaparib by using the PROTAC approach [1]. Pomalidomide 4'-PEG3-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-159452
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Azide
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SMARCA2/4-degrader-1 (compound I-430) 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 [1].
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- HY-159777
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Alkynes
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CPI-203-PEG5-Alkyne is a conjugate of E3 ligase and linker. CPI-203-PEG5-Alkyne can be used for synthesis of PROTAC BRD4-DCAF1 degrader-1 (HY-169151) [1].
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- HY-163647
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Azide
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Lenalidomide-COCH-PEG2-azido is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based cereblon ligand and a linker. Lenalidomide-COCH-PEG2-azido can be used in the synthesis of PROTAC AKR1C3 degrader-1 (HY-163609) [1].
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- HY-130984
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PROTAC Synthesis
Azide
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Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker. Azido-PEG1-CH2COO-Cl can be used in the synthesis of PROTAC BRD4 Degrader-1 (HY-133131) [1]. Azido-PEG1-CH2COO-Cl 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-W457949
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Azide
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Pomalidomide 4'-alkylC4-azide (Compound 2) is an azide compound containing a MIDI group and is one of the compounds used to construct a library of MIDI azide compounds. Pomalidomide 4'-alkylC4-azide can be used to develop research on PROTAC degraders .
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- HY-151792
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Azide
PROTAC Synthesis
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Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. Pomalidomid-C6-PEG3-butyl-N3 also is a crosslinker-E3 ligase ligand conjugate, which be used in click reactive protein degrader building block for PROTAC research.
Pomalidomid-C6-PEG3-butyl-N3 also can be used in the template for synthesis of targeted protein degrader . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
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