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Results for "

Heterobifunctional Molecules

" in MedChemExpress (MCE) Product Catalog:

14

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-145232
    PhosTAC7
    3 Publications Verification

    		 Phosphatase Tau Protein Neurological Disease Cancer
    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) .
    PhosTAC7
  • HY-128925
    AMAS
    1 Publications Verification

    		 ADC Linker Cancer
    AMAS is a nonclaevable heterobifunctional crosslinker with NHS ester and maleimide groups that allows covalent conjugation of amine- and sulfhydryl-containing molecules.
    AMAS
  • HY-147098
    dTAG-47

    		PROTACs FKBP Cancer
    dTAG-47 is a FKBP12F36V PROTAC degrader. dTAG-47 efficiently degrades FKBP12F36V-MELK(sg3R) in MELK ⁻/⁻ MDA-MB-468-FKBP12F36V-MELK(sg3R) cells. dTAG-47 can be used for the research of basal-like breast cancers (BBC). (Pink: FKBP12F36V ligand (HY-114420), Blue: CRBN Ligand (HY-W087383), Black: Linker (HY-42773), E3 ligase ligand-linker conjugate (HY-175952)) .
    dTAG-47
  • HY-156820
    HLDA-221

    		Epigenetic Reader Domain Cancer
    HLDA-221 is a heterobifunctional small molecules called Regulated Induced Proximity Targeting Chimeras (RIPTACs). HLDA-221 elicits a stable ternary complex between a target protein selectively expressed in cancer tissue and a pan-expressed protein essential for cell survival, thus leading to cell death selectively in cells expressing the target protein .
    HLDA-221
  • HY-138642
    Vepdegestrant
    3 Publications Verification

    ARV-471

    		 PROTACs Estrogen Receptor/ERR Cancer
    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 .
    Vepdegestrant
  • HY-163677
    ARM165

    		PROTACs PI3K Akt Cancer
    ARM165 is a heterobifunctional molecule. ARM165 degrades the PIK3CG proteins, inhibits PI3Kγ-Akt signaling pathway, and thus exhibits antileukemia efficacy. ARM165 inhibits proliferations of AML cells, with IC50 <1 μM. (Pink: ligand for target protein PI3Kγ inhibitor AZ2 (HY-111570); Black: linker; Blue: ligand for E3 ligase Pomalidomide (HY-10984))
    ARM165
  • HY-134850
    QC-01–175

    		PROTACs Tau Protein Neurological Disease
    QC-01-175 is a heterobifunctional molecule, which degrades aberrant tau. QC-01-175 reduces the levels of A152T and P301L mutant tau protein and protects neurons from tau-mediated toxicity and improve cell survival (Pink: ligand for target protein Aberrant tau ligand 1 (HY-W453397); Black: linker NH2-PEG3 (HY-W007545); Blue: ligand for E3 ligase Pomalidomide (HY-10984)) .
    QC-01–175
  • HY-129655
    Sulfo-SMPB sodium

    		ADC Linker Cancer
    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 .
    Sulfo-SMPB sodium
  • HY-138642A
    (Rac)-Vepdegestrant

    (Rac)-ARV-471

    		 Estrogen Receptor/ERR PROTACs Cancer
    (Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) 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 .
    (Rac)-Vepdegestrant
  • HY-W1005067
    EN171

    		Molecular Glues Hippo (MST) Estrogen Receptor/ERR Others
    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 .
    EN171
  • HY-176501
    FKBP12 ligand-2

    		FKBP Cancer
    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 .
    FKBP12 ligand-2
  • HY-161769
    HL435

    		PROTACs Epigenetic Reader Domain Apoptosis Cancer
    HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
    HL435
  • HY-176502
    FKBP12 ligand-3

    		FKBP Cancer
    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 .
    FKBP12 ligand-3
  • HY-145925B
    CFT8634
    1 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    CFT8634 is an orally bioavailable PROTAC BRD9 targeted degrader based on the E3 ubiquitin ligase CRBN mechanism. CFT8634 can be used for the study of synovial sarcoma and SMARCB1-deficient solid tumors (Pink: BRD9 ligand (HY-169988); Blue: E3 ligase ligand (HY-169989); Black: linker (HY-169991). CFT8634 is a heterobifunctional molecule that binds to BRD9 at one end and recruits CRBN at the other end, which can inhibit the growth of tumor cells that depend on BRD9. CFT8634 can be used for the study of SMARCB1-related cancers (such as synovial sarcoma and malignant rhabdoid tumor) .
    CFT8634

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