Search Result
Results for "
Degrader-1
" in MedChemExpress (MCE) Product Catalog:
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-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-162331
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STING
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Inflammation/Immunology
Cancer
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STING Degrader-1 (compound 2) is a potent STING degrader that covalently binds to STING and E3 ligase. STING Degrader-1 induces STING degradation through a ubiquitin-proteasome system-dependent pathway [1].
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- HY-153368
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IRAK
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Cancer
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IRAK degrader-1 (example I-3) is a potent IRAK degrader .
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- HY-147656
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NAMPT
Autophagy
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Cancer
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NAMPT degrader-1 (Compound A3) 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-W248665A
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Androgen Receptor
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Cancer
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Androgen receptor degrader-1 (compound 18) is a potent androgen receptor degrader. Androgen receptor degrader-1 can be used in research of cancer [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-128845
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PROTACs
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Cancer
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PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader .
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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-150608
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STING
PROTACs
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Inflammation/Immunology
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PROTAC STING Degrader-1 (Compound SP23) is a STING PROTAC degrader with a DC50 of 3.2 μM. PROTAC STING Degrader-1 shwos anti-inflammatory activity [1].
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- HY-156401
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Epigenetic Reader Domain
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Cancer
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BRD9 Degrader-1 is a BRD9 degrader. BRD9 Degrader-1 exhibits micromolar binding affinity to BRD9 and nanomolar affinity for the ternary complex with BRD9 and VCB [1].
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- HY-162014
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PROTACs
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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-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-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-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-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-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-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-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-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-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-155552
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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. GSPT1 degrader-1 also induces cell G0/G1 phase arrest and apoptosis [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-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-132998
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PROTACs
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Others
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HDAC6 degrader-1 is a PROTAC that comprises a selective HDAC6 inhibitor Nexturastat A (Nex A) as the HDAC6 binder, a linker and a ligand for recruiting E3 ligase. HDAC6 degrader-1 induces significant degradation of HDAC6, exhibits excellent selectivity against other HDACs, and demonstrates efficient inhibition of cell proliferation [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-111844
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SNIPERs
PROTACs
RAR/RXR
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Cancer
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PROTAC RAR Degrader-1 comprises a IAP ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) [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-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-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-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-128840
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PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
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Cancer
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PROTAC MDM2 Degrader-1 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase (CN108610333A) [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-145737A
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PROTACs
Ras
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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-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-155643
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PROTACs
Glutaminase
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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
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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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Others
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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-163152
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- HY-103628
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PROTACs
CDK
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Cancer
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PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.
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- HY-157427
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PROTACs
Polo-like Kinase (PLK)
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Cancer
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PROTAC PLK1 Degrader-1 (DD-2) is a potent PROTAC PLK1 degrader. PROTAC PLK1 Degrader-1 selectively induces PLK1 degradation in cancer cells, including HeLa (DC50=2.5 μM) and nonsmall cell lung cancer (NSCLC), through the N-degron pathway [1].
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- HY-125877
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PROTACs
Bcl-2 Family
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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-155008
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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].
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- HY-146324
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PROTACs
CaMK
Apoptosis
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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-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-138536
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PROTACs
Epigenetic Reader Domain
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Cancer
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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-131188
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PROTACs
Bcl-2 Family
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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-149845
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GSK-3
PROTACs
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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-144657
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PROTACs
Ras
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Cancer
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(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)
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Inflammation/Immunology
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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-160262
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- HY-145071
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PROTACs
Estrogen Receptor/ERR
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Cancer
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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-149236
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- HY-130709
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PROTACs
CDK
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Cancer
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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-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-148521
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CDK
FLT3
PROTACs
Apoptosis
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Cancer
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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-151110
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PROTACs
CDK
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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-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-139186
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PROTACs
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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-144657A
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PROTACs
Ras
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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-137487
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PROTACs
Raf
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Cancer
|
|
PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value 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). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth [1].
|
-
- HY-147525
-
|
|
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].
|
-
- HY-130612
-
|
|
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-145479
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM [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-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-129966
-
|
|
PROTACs
IRAK
|
Cancer
|
|
PROTAC IRAK4 degrader-1 is a Cereblon-based PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively [1].
|
-
- 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-125878
-
|
SGK3-PROTAC1
|
PROTACs
SGK
|
Cancer
|
|
PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on von Hippel-Lindau ligand. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate) [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-157304
-
|
|
Atg8/LC3
ATTECs
Autophagy
Mitophagy
|
Neurological Disease
|
|
ATTECs Degrader 1 (Compound MT1) is an ATTECs compound. ATTECs Degrader 1 can bind to both the outer mitochondrial membrane protein (TSPO) and the autophagosome protein LC3B. ATTECs Degrader 1 enhances the degradation of damaged mitochondria by autophagosomes and subsequent autophagic degradation .
|
-
- HY-155582
-
|
|
Others
|
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-149917
-
|
|
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). 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 also shows good plasma exposure levels [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-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-157458
-
|
|
ATTECs
Phosphodiesterase (PDE)
Autophagy
|
Cancer
|
|
PDEδ autophagic degrader 1 (compound 12c) 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-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-130245
-
|
|
Ser/Thr Protease
|
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-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-161168
-
|
|
CDK
|
Cancer
|
|
Cyclin K degrader 1 (compound 40) is an AT7519 (HY-50940) based Cyclin K degrader with DC50 of 21 nM [1].
|
-
- HY-119932
-
|
|
PROTACs
FAK
|
Cancer
|
|
PROTAC FAK degrader 1 is a selective and potent von Hippel-Lindau-based focal adhesion kinase (FAK) degrader with an IC50 of 6.5 nM, DC50 of 3 nM [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-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-162282
-
|
|
DNA Methyltransferase
|
Cancer
|
|
PROTAC METTL3-14 degrader 1 (compound 29) is a PROTAC degrader of METTL3-14. PROTAC METTL3-14 degrader 1 shows a 50% or higher degradation of METTL3 and/or METTL14 [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-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-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-114323
-
|
|
PROTACs
FLT3
Apoptosis
|
Cancer
|
|
PROTAC FLT-3 degrader 1 is a von Hippel-Lindau-based PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction [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-161176
-
|
|
PROTACs
|
Cancer
|
|
PROTAC KRAS G12D degrader 1 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-161101
-
-
- HY-162318
-
|
|
c-Myc
|
Cancer
|
|
A80.2HCl is a MYC degrader that restores pRB1 protein activity and reduces MYC-dependent CDK4/6 resistance. A80.2HCl has antitumor activity [1].
|
-
- HY-147654
-
|
|
PROTACs
Influenza Virus
|
Infection
|
|
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].
|
-
- 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-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-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-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-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-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
-
|
|
IKZF Family
|
Cancer
|
|
IKZF1-degrader-1 (Compound 9-B) is a degrader to IKZF1 protein, with DC50 value of 0.134 nM. IKZF1-degrader-1 can be used to degrader tumors [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-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-W087383
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide 5-fluoride is Thalidomide-based cereblon ligand that incorporates to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-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-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-130814
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
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-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-130852
-
-
- 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-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-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-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-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-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-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-149924
-
|
|
PROTACs
IAP
|
Cancer
|
|
CST626 (Compound 9) is a pan-IAP degrader PROTAC. PROTAC pan-IAP degrader-1 degrades XIAP, cIAP1 and cIAP2 with DC50s of 0.7, 2.4, and 6.2 nM in MM.1S cells, respectively [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-41547
-
|
Cereblon ligand 4; E3 ligase Ligand 4
|
Ligands for E3 Ligase
|
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-130813
-
-
- 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-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-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-130713
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-C2-amido-C2-COOH incorporates a CRBN ligand for the E3 ubiquitin ligase, and a linker. Thalidomide-C2-amido-C2-COOH can be used to design PROTAC CDK2/9 Degrader-1 (HY-130709) [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-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-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-130815
-
-
- HY-130815A
-
-
- 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-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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur 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-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-156745
-
-
- HY-156746
-
-
- HY-137343
-
-
- HY-156744
-
-
- HY-156747
-
-
- HY-N8180
-
|
|
Others
|
Others
|
|
Silyamandin is a flavonolignan compound. Silydianin can form Silyamandin through oxidative degradation .
|
-
- HY-155398
-
-
- HY-155397
-
-
- HY-157763
-
|
|
PROTACs
Btk
|
Cancer
|
|
PROTAC BTK Degrader-8 (compound 3) is a potent PROTAC BTK degrader .
|
-
- HY-150859
-
|
|
HDAC
|
Cancer
|
|
HDAC ligand-1 is a HDAC ligand that can be used to synthesize PROTAC HDAC degraders .
|
-
- HY-113136
-
|
N1-Methylguanosine
|
Endogenous Metabolite
|
Cancer
|
|
1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker [1].
|
-
- HY-W584512
-
|
|
Others
|
Others
|
|
Thalidomide-NH-CH2-COO (t-Bu) is a molecular block of small-molecule degrader .
|
-
- HY-157582
-
|
|
Others
|
Others
|
|
MS39N (compound 27) is a negative control for MS39 that binds EGFR without inducing degradation .
|
-
- HY-143346
-
|
|
Others
|
Cancer
|
|
CCW16 is the covalent ligand for the E3 ubiquitin ligase RNF4. CCW16 can be used in the synthesis of protein degraders .
|
-
- HY-150400
-
-
- HY-153042
-
|
|
Others
|
Others
|
|
Thalidomide-NH-C2-azaspiro[3.5]nonane hydrochloride is an intermediate that can be used to synthesize irak degrader .
|
-
![Thalidomide-NH-C2-azaspiro[3.5]nonane hydrochloride](//file.medchemexpress.com/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
-
|
|
|
|
|
Steviol is a major metabolite of the sweetening compound stevioside. Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation .
|
-
- HY-139340
-
|
|
Others
|
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-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-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-130640
-
-
- HY-118653
-
|
|
MAGL
|
Metabolic Disease
|
|
SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation .
|
-
- HY-141551B
-
|
|
Others
|
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-W017389
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
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-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-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-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-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-113136S
-
|
N1-Methylguanosine-d3
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Others
|
|
1-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.
|
-
- HY-160438
-
|
|
Others
|
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-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-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-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-157592
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
MMH2-NR a negtive control of MMH2. MMH2 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader .
|
-
- HY-129363
-
-
- HY-148523
-
|
|
Others
|
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-N7045
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) 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-156395
-
|
|
Others
|
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-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-126534
-
-
- 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-130800
-
-
- HY-157591
-
|
|
Others
|
Others
|
|
MMH1-NR, containing a non-reactive (ethyl) group is a negative control of MMH1. MMH1 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader .
|
-
- HY-130648
-
-
- HY-13822
-
SKI II
2 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-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-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-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-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-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-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-163168
-
|
CFT-4531
|
DNA/RNA Synthesis
|
Cancer
|
|
aTAG 4531 (CFT-4531) is a potent, selective, and onmechanism tool degrader of MTH1 with DC50 value of 0.28 nM and Ki value of 1.8 nM.
degradation activity is due to the intricate formation of the ternary complex between the MTH1 aTAG, CRBN E3 ligase, and aTAG tool degrader .
|
-
- HY-13982
-
JSH-23
Maximum Cited Publications
80 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-133017
-
|
SAR439859
|
Estrogen Receptor/ERR
|
Cancer
|
|
SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation . SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER + breast cancer .
|
-
- 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-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-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-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-141894
-
|
|
Others
|
Others
|
|
5-Ph-IAA-AM is an eggshell-permeable 5-Ph-IAA analog. 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-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-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[1][2].
|
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- HY-157765
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PROTACs
Estrogen Receptor/ERR
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Cancer
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PROTAC ERα Degrader-6 (compound A3) is a potent PROTAC degrader of ERα, with DC50 of 0.12 μM. 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 .
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- HY-114407
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PROTACs
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-N6769
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Monorden
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HSP
Bacterial
Antibiotic
Parasite
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Infection
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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 .
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- HY-111836
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Molecular Glues
β-catenin
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Cancer
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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 .
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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-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-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-151792
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PROTACs
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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 .
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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-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-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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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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[1][2].
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- HY-113136S
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1-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.
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| Cat. No. |
Product Name |
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Classification |
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- HY-133138
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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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-130984
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Azide
PROTAC Synthesis
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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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur 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
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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 .
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- HY-130652
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Azide
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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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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