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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
18 Results for "
Heterobifunctional Molecules
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "Heterobifunctional Molecules" in MCE Product Catalog:
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6 Publications Verification
Synonyms: ARV-471; PF-07850327
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Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
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PhosTAC7 is a heterobifunctional molecule named as a Phosphorylation Targeting Chimera (PhosTAC). PhosTAC7 can dephosphorylate the PDCD4 protein, FOXO3a protein, and tau protein by recruiting serine/threonine protein phosphatase 2A (PP2A). PhosTAC7 offers the advantage of selectively modulating the phosphorylation state of individual target proteins, making it a promising tool for research in cancer and tau protein-related neurodegenerative diseases (Alzheimer's disease) .
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1 Cited Publications
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AMAS is a nonclaevable heterobifunctional crosslinker with NHS ester and maleimide groups that allows covalent conjugation of amine- and sulfhydryl-containing molecules.
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dTAGV-1-NEG is an inactive FKBP12 F36V PROTAC degrader, the diastereomer of dTAGV-1 (HY-145514D), and a heterobifunctional negative control molecule. dTAGV-1-NEG does not degrade any protein .
Cat. No.: HY-W588706
Cat. No.: HY-W1005067
CAS No.: 2191110-79-7
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EN171 is a covalent ligand that covalently targets both C38 and C96 on 14-3-3 to enhance 14-3-3 interactions with ERα, YAP and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity. EN171 can not only be used as a molecular glue to enhance native protein interactions but can also be used as a covalent 14-3-3 recruiter in heterobifunctional molecules to sequester nuclear neo-substrates such as BRD4 and BLC6 into the cytosol .
Cat. No.: HY-158408
CAS No.: 3062992-25-7
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NZ-66 is a ULK1-Recruiting Chimera (ULKREC) and heterobifunctional chimeric molecule composed of a BL-918-derived ULK1 agonist linked to a mitochondrial outer membrane-targeting TSPO ligand via a six-carbon hexane linker. NZ-66 is a mitophagy inducer recruits ULK1 to mitochondria to induce ULK1-dependent mitophagy, enhanced by mitochondrial insult, independently of the PRKN/PINK axis. NZ-66 can be used for the research of parkinson’s disease .
Cat. No.: HY-161130
CAS No.: 2624336-87-2
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Lenalidomide 4'-PEG3-amine dihydrochloride is a lenalidomide (HY-A0003)-derived immunomodulator and monofunctional synthetic intermediate, as well as a E3 ubiquitin ligase ligand. Lenalidomide 4'-PEG3-amine dihydrochloride can be used for the preparation of small-molecule drug conjugates and heterobifunctional protein degraders .
Cat. No.: HY-138642S
CAS No.: 3025452-07-4
Synonyms: ARV-471-d5 PF-07850327-d5
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Vepdegestrant-d5 (ARV-471-d5) is the deuterium labeled Vepdegestrant (HY-138642). Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a DC50 of about 2 nM .
Cat. No.: HY-176130
CAS No.: 3115333-82-6
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MRL828 is a heterobifunctional molecule that targets aggregated tau protein. As an autophagy-targeting chimera (ATTEC), MRL828 selectively labels aggregated tau protein for clearance via the autophagy (autophagy)-lysosome pathway. The activity of MRL828 depends on autophagosomes rather than lysosomes, and it induces autophagosome-dependent secretion. MRL828 acts as an intracellular aggregate inhibitor and a secretory autophagy inducer, reducing intracellular levels of aggregated tau protein through autophagosome-dependent secretory autophagy instead of lysosomal degradation. MRL828 can be used in the research of neurodegenerative diseases such as Alzheimer's disease .
Cat. No.: HY-176502
CAS No.: 3036374-26-9
FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels .
Cat. No.: HY-129655
CAS No.: 92921-26-1
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Sulfo-SMPB sodium is a non-cleavable, heterobifunctional chemical cross-linking reagent which contains N-hydroxysuccinimide (NHS) ester and maleimide groups, allowing covalent conjugation of amine- and sulfhydryl-containing molecules .
Cat. No.: HY-145514B
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dTAGV-1-NEG TFA is an inactive FKBP12 F36V PROTAC degrader, the diastereomer of dTAGV-1 (HY-145514D), and a heterobifunctional negative control molecule. dTAGV-1-NEG TFA does not degrade any protein .
Cat. No.: HY-138642A
CAS No.: 2229711-08-2
Synonyms: (Rac)-ARV-471; (Rac)-PF-07850327
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(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
Cat. No.: HY-176501
CAS No.: 3036243-81-6
FKBP12 ligand-2 (compound d) is a high affinity ligand targeting FKBP12. FKBP12 ligand-2 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-2 can be used for selective cancer research based on differences in intracellular presenter protein levels .
Cat. No.: HY-182577
CAS No.: 2154350-81-7
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CFT-743, a PROTAC-based heterobifunctional degrader and BET inhibtor, is a degrader of BRD4 bromodomain 1 (BD1) with a DC50 of 4.3 nM. CFT-743's antitumor activitiy is dependent on BET degradation and can be attenuated by Pomalidomide (HY-10984), which is a CRBN binding molecule. CFT-743 induces ubiquitination of BRD4 BD1. CFT-743 can be used for cancer research .
Cat. No.: HY-183439
CAS No.: 2365116-48-7
dTAG-Fluorescein is a fluorescent acceptor probe and heterobifunctional proteolysis targeting chimeric molecule (PROTAC) .dTAG-Fluorescein functions in Homogeneous Time Resolved Fluorescence (HTRF) competitive displacement binding assays to measure binding affinity to His-FKBP12(F36V) .dTAG-Fluorescein recruits von Hippel-Lindau or CRBN E3 ligase complexes to drive selective degradation of FKBP12 F36V-tagged proteins, with limited activity towards FKBP12 WT and IKZF1 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
