Search Result
Results for "
PROTAC K-Ras degrader
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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 .
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- HY-168054
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PROTACs
Ras
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Cancer
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PROTAC K-Ras Degrader-3 (compound 40) is a PROTAC degrader of K-Ras with a DC50 of ≤ 1 nM against SW620 KRAS G12D, and a GI50 of ≤ 10 nM against SW620 3D cell growth. PROTAC K-Ras Degrader-3 can be utilized in cancer research .
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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 . (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-153821
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Ras
PROTACs
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Cancer
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PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS .
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- HY-164365
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PROTACs
Ras
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Cancer
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PROTAC K-Ras degrader-2 (compound 48) is a pan-KRAS-mutant PROTAC degrader with an IC50 of ≤200 nM for KRAS G12V/RAF1. PROTAC K-Ras degrader-2 degrades SW620 KRAS G12D with a DC50 of ≤200 nM. PROTAC K-Ras degrader-2 inhibits cell growth of SW620 3D cell with an IC50 of ≤20 nM. (Pink: KRAS inhibitor-30 (HY-164366)) .
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- HY-168669
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PROTACs
Ras
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Cancer
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pan-KRAS degrader 4 (compound 69) is a potent cereblon-based KRAS PROTAC degrader, with a DC50 of <100 nM. pan-KRAS degrader 4 shows anticancer effects. (Pink: ligand for target protein (HY-168671); Black: linker (HY-168670); Blue: E3 ligase ligand (HY-W733895)) .
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- HY-168678
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PROTACs
Ras
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Cancer
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pan-KRAS degrader 5 (compound 102) is a potent cereblon-based KRAS PROTAC degrader, with a DC50 of <100 nM. pan-KRAS degrader 5 shows anticancer effects. (Pink: ligand for target protein (HY-168679); Black: linker (HY-168670); Blue: E3 ligase ligand (HY-W580113)) .
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- HY-129776
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Target Protein Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-129775
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Target Protein Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-130991
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Target Protein Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-176489
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PROTACs
Ras
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Cancer
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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 . Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligase ligand (HY-170353); Black: linker (HY-176491);
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- HY-139186
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PROTACs
Ras
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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 .
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- HY-161176
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PROTACs
Ras
ERK
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Cancer
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PROTAC KRAS G12D degrader 1 is a selective PROTAC KRAS G12D degrader. PROTAC KRAS G12D degrader 1 inhibits proliferation of KRAS G12D-mutant cells and suppresses ERK phosphorylation. PROTAC KRAS G12D degrader 1 inhibits tumor growth in mice bearing AsPC-1 xenografts. PROTAC KRAS G12D degrader 1 can be used for the study of KRAS G12D-driven cancers.(Pink: KRAS ligand (HY-175892), Blue: VHL Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175893)) .
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- HY-161177
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PROTACs
Ras
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Infection
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PROTAC KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPro). Protac KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPRO). The PROTAC molecule is designed by partially coupling a GC-376-based dipeptidyl 3CLPro ligand with pomadomide via a piperazine-piperidine linker .
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- HY-168056
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Others
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Others
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KRAS ligand 5 is the target protein ligand for PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can specifically degrade KRAS mutated proteins .
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- HY-130707
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Target Protein Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-130991A
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Target Protein Ligand-Linker Conjugates
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Cancer
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K-Ras ligand-Linker Conjugate 6 formate 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 formate 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 .
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- HY-130822
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Target Protein Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-130823
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Target Protein Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-168055
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Ligands for E3 Ligase
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Cancer
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(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 .
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- HY-130819
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PROTAC Linkers
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Cancer
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Tos-PEG4-THP is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523) .
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- HY-130821
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PROTAC Linkers
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Cancer
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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) .
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- HY-130820
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PROTAC Linkers
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Cancer
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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) .
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- HY-168075
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PROTAC Linkers
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Others
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Boc-PIP-Me-CH2-2,7-diazaspiro[3.5]nonane is the linker of PROTAC K-Ras Degrader-3 (HY-168054), which can be used in the synthesis of PROTACs .
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- HY-168076
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PROTAC-Linker Conjugates for PAC
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Cancer
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(S)-Deoxy-thalidomide-2,7-diazaspiro[3.5]nonane-CH2-Me-PIP-Boc consists of E3 ligase ligand and PROTAC linker of PROTAC K-Ras Degrader-3 (HY-168054). (S)-Deoxy-thalidomide-2,7-diazaspiro[3.5]nonane-CH2-Me-PIP-Boc is promising for research of cancers .
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- HY-145615
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-176490
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- HY-168671
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- HY-176792
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PROTACs
Ras
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Cancer
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ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader. ACBI-4 has significant anti-proliferative effect and potently degrades multiple KRAS mutants in cancer cells, such as KRASG12R .
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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 .
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- HY-176491
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PROTAC Linkers
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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) .
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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 .
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- HY-176134
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PROTACs
Ras
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Cancer
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RP03707 is a PROTAC based KRAS G12D degrader (Red: KRAS G12D inhibitor (HY-134813), black: linker, Blue: E3 ligase ligand) .
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- HY-175860
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Target Protein Ligand-Linker Conjugates
Ras
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Cancer
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KRAS G12D ligand-Linker Conjugate 2 is a conjugate of the KRAS (G12D) ligand (HY-175859) and the linker (HY-168698). KRAS G12D ligand-Linker Conjugate 2 can be used for synthesizing PROTAC KRAS (G12D) degrader ASP-3082 (HY-157505) .
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- HY-157228
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PROTACs
Ras
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Cancer
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ACBI3 (compound 7), a chemical probe, 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 .
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- HY-139403
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Target Protein Ligand-Linker Conjugates
Ras
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Cancer
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MRTX849 ethoxypropanoic acid incorporates a ligand for KRAS G12C, and a PROTAC linker. MRTX849 ethoxypropanoic acid can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (IC50s between 0.25 and 0.76 μM) .
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- HY-137516
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LC-2
2 Publications Verification
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PROTACs
Ras
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Cancer
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LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM . LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines .
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- HY-173252
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Ligands for Target Protein for PROTAC
Ras
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Cancer
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KRASG12C ligand-1 is a PROTAC target protein ligand that can be used to synthesize the PROTAC YN14-H (HY-173250). YN14-H is a PROTAC degrader targeting KRAS G12C and has antitumor activity .
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- HY-168672
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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E3 Ligase Ligand-linker Conjugate 133 is a conjugate of E3 ligase ligand and linker that serve as a key intermediate for the synthesis of complete PROTAC molecule pan-KRAS degrader 4 (HY-168669) .
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- HY-168680
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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E3 Ligase Ligand-linker Conjugate 135 is a conjugate of E3 ligase ligand and linker that serve as a key intermediate for the synthesis of complete PROTAC molecule pan-KRAS degrader 5 (HY-168678) .
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- HY-161654
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SOS1
PROTACs
Ras
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Cancer
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PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC50s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC50s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655); Black: linker (HY-161656); Blue: E3 ligase ligand (HY-W249500))
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- HY-148273
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ASP-3082; KRas G12D inhibitor 17
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PROTACs
Ras
ERK
Akt
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Cancer
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Setidegrasib (KRAS G12D inhibitor 17, ASP3082) is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib suppresses p-ERK, p-AKT, p-S6 levels in AsPC-1 cells. Setidegrasib exhibits anti-tumor activity in various cancer xenograft models in mice. Setidegrasib can be used for the study of KRAS(G12D)-mutated solid tumors. (Blue: VHL ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700)) .
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- HY-144323
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PROTACs
PERK
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Cancer
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YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .
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- HY-162281
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PROTACs
SOS1
Ras
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Cancer
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PROTAC SOS1 degrader-6 (compound 23) is an effective SOS1 PROTACs degrader that synergizes with KRAS G12C inhibitors . PROTAC SOS1 degrader-6 consists of the target protein ligand (red part) SOS1 Ligand intermediate-7 (HY-169371), E3 ubiquitin ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and PROTAC linker (black part) 5-Bromopentanoic acid (HY-W016456). Among them, the E3 ubiquitin ligase ligand + linker can form (S,R,S)-AHPC-CO-C4-bromine (HY-169372).
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- HY-139402
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Ras
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Cancer
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MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM) .
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- HY-161233
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SOS1
PROTACs
ERK
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Cancer
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BTX-6654 is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations .
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- HY-176492
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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) .
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- HY-W998345
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PROTACs
PDK-1
Akt
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Cancer
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SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models.(Blue: CRBN ligand; Black: linker; Pink: Smurf1 ligand (Smurf1-L)) .
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- HY-176786
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PROTACs
Ras
Apoptosis
PERK
p38 MAPK
Caspase
TNF Receptor
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Cancer
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MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .
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- HY-168637
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SOS1
PROTACs
Ras
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Cancer
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SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a Kd of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRAS G12C or KRAS G12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity. (Pink: SOS1 ligand (HY-168638); Black: linker (HY-W539874); Blue: E3 ligase ligand (HY-W076696)) .
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- HY-161450
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PROTACs
Ras
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Cancer
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LHF418 is an effective SOS1 PROTAC degrader with a DC50 value of 209.4 nM in A549 cells. LHF418 can effectively inhibit RAS signaling and colony formation in KRAS-driven cancer cells. (Structural note: (Blue: Cereblon ligand (HY-A0003), Black: linker; Pink: SOS1 binder SOS1 Ligand intermediate-3 (HY-161452)) .
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- HY-175025
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PROTACs
Ras
Apoptosis
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Cancer
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CH091138 is a potent and selective KRASG12D PROTAC degrader with DC50s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRAS WT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)) .
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- HY-173250
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PROTACs
Ras
Apoptosis
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Cancer
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YN14-H is a PROTAC degrader targeting KRAS G12C. YN14-H inhibits cell growth in NCI-H358 and MIA PaCa-2 cells (IC50 values of 0.042, 0.021 μM, DC50 values of 28.9, 18.1 nM, respectively). YN14-H significantly induces apoptosis and inhibits migration. YN14-H demonstrates favorable pharmacokinetic properties and excellent antitumor activity in vivo. (Structure Note: Pink: target protein ligand (HY-173252); Blue: E3 ligase ligand (HY-125905); Black: linker (HY-Y0840); E3 ligase ligand + linker (HY-173253) .
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Product Name |
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Classification |
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- HY-175860
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Alkynes
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KRAS G12D ligand-Linker Conjugate 2 is a conjugate of the KRAS (G12D) ligand (HY-175859) and the linker (HY-168698). KRAS G12D ligand-Linker Conjugate 2 can be used for synthesizing PROTAC KRAS (G12D) degrader ASP-3082 (HY-157505) .
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