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Results for "

small molecule degradation

" in MedChemExpress (MCE) Product Catalog:

39

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2

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1

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-115865
    XIAP degrader-1
    1 Publications Verification

    IAP Cancer
    XIAP degrader-1, a primary amine tethered small molecule, promotes the degradation of X-linked inhibitor of apoptosis protein (XIAP).
    XIAP degrader-1
  • HY-145514C

    FKBP PROTACs Cancer
    dTAGV-1 hydrochloride is the hydrochloride form of dTAGV-1 that is a small molecule degrader of FKBP12 .
    dTAGV-1 hydrochloride
  • HY-144984

    Others Cancer
    NRX-1933 is a β-catenin:β-TrCP interaction enhancer for the development of small molecule degraders.
    NRX-1933
  • HY-155021

    PROTACs α-synuclein Neurological Disease
    PROTAC α-synuclein degrader 5 is a highly selective small-molecule degraders (PROTAC) of α-synuclein aggregates, with an DC50 of 7.51 μM and the highest degradation rate Dmax of 89%. PROTAC α-synuclein degrader 5 contains probe molecule sery308 and E3 ligase ligands. PROTAC α-synuclein degrader 5 can be used for neurological disease research .
    PROTAC α-synuclein degrader 5
  • HY-146324

    PROTACs CaMK Apoptosis Cancer
    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 .
    PROTAC eEF2K degrader-1
  • HY-111556
    BSJ-03-123
    4 Publications Verification

    PROTACs CDK Cancer
    BSJ-03-123 is a PROTAC connected by ligands for Cereblon and CDK as a potent and novel CDK6-selective small-molecule degrader.
    BSJ-03-123
  • 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 .
    TCH-165
  • HY-142881

    LYTACs Others
    D-MoDE-A (1) is a bifunctional small molecule that mediates the degradation of extracellular proteins through the asialoglycoprotein receptor (ASGPR).
    D-MoDE-A (1)
  • HY-142885

    LYTACs Others
    M-MoDE-A (2) is a bifunctional small molecule that mediates the degradation of extracellular proteins through the asialoglycoprotein receptor (ASGPR).
    M-MoDE-A (2)
  • HY-W584512

    Others Others
    Thalidomide-NH-CH2-COO (t-Bu) is a molecular block of small-molecule degrader .
    Thalidomide-NH-CH2-COO(t-Bu)
  • HY-131203

    Epigenetic Reader Domain Apoptosis c-Myc Caspase Cancer
    PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4 degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research .
    PROTAC BRD4 Degrader-6
  • HY-117878

    Others Metabolic Disease
    ML345 is a potent and selective insulin-degrading enzyme (IDE) small-molecule inhibitor, with an IC50 value of 188 nM. ML345 can be for use as a pharmacophore for agent development in diabetes research .
    ML345
  • HY-151227

    Others Cancer
    VL285 Phenol is a VL285 analogue with Phenol group. VL285, a small molecule VHL ligand, can be served as a degrader for HaloPROTAC3 synthesis.VL285 degrades HaloTag7 fusion proteins (IC50=0.34 μM) .
    VL285 Phenol
  • HY-130245

    PCSK9 Metabolic Disease
    PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor .
    PCSK9 degrader 1
  • HY-156730A

    Molecular Glues STAT Cancer
    KT-333 ammonium (Compound A) is a molecular glues that degrades STAT3 protein. KT-333 ammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 ammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 ammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
    KT-333 ammonium
  • HY-156730

    Molecular Glues STAT Cancer
    KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
    KT-333
  • HY-156730B

    Molecular Glues STAT Cancer
    KT-333 diammonium is a molecular glues that degrades STAT3 protein. KT-333 diammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 diammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 diammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
    KT-333 diammonium
  • HY-130245A

    PCSK9 Metabolic Disease
    (R,R)-PCSK9 degrader 1 is the isomer of PCSK9 degrader 1 (HY-130245). PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor .
    (R,R)-PCSK9 degrader 1
  • HY-147102

    LYTACs Cancer
    tri-GalNAc biotin is a small molecule lysosome targeting degrader. tri-GalNAc is a ligand of ASGPR (asialoglycoprotein receptor). tri-GalNAc biotin can facilitate the uptake of NeutrAvidin (NA) through ASGPR in liver cells. tri-GalNAc biotin delivers NeutrAvidin to lysosome for degradation. tri-GalNAc biotin can be used for research of LYsosome TArgeting Chimera (LYTAC) .
    tri-GalNAc biotin
  • HY-400766

    Others Cancer
    BWA-522 intermediate-2 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .
    BWA-522 intermediate-2
  • HY-401056

    Others Cancer
    BWA-522 intermediate-3 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .
    BWA-522 intermediate-3
  • HY-162562

    PCSK9 Cardiovascular Disease
    E28362 is a novel small molecule PCSK9 inhibitor. E28362 blocks the interaction between PCSK9 and LDLR, thereby preventing the degradation of LDLR and maintaining cholesterol homeostasia. E28362 is a promising lead compound for the study of hyperlipidemia and atherosclerosis .
    E28362
  • HY-W877989

    Ligands for E3 Ligase Cancer
    BWA-522 intermediate-1 is an intermediate in the synthesis of PROTAC BWA-522 (HY-149433) and serves as a ligand molecule for cereblon E3 ubiquitin ligase. BWA-522 is an orally active small molecule protein-targeting chimera (PROTAC) that has significant degradation effects on AR-FL and AR-V7 .
    BWA-522 intermediate-1
  • 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 .
    PEG6-(CH2CO2H)2
  • HY-113646

    FKBP Others
    Shield-2 is an efficient stabilizing ligand binding to the FKBP (F36V) protein with a dissociation constant of 29 nM. Shield-2 binds tightly to the FKBP mutants destabilizing domains and prevents degradation, thus providing small molecule regulation over intracellular protein levels .
    Shield-2
  • HY-167680

    GSK823093

    Others Metabolic Disease
    Denagliptin (GSK823093) is a small molecule dipeptidyl peptidase IV (DPP-4) inhibitor with activity for the suppression of endocrine and metabolic diseases. Denagliptin can be used to study type 2 diabetes. Denagliptin is stable in the solid state but degrades in solution and in mixtures with various excipients. Denagliptin also exhibits degradation in capsules, mainly through cyclization reactions to form (3S,7S,8aS) aminoamines to provide further synthetic materials. The degradation pathway of Denagliptin was elucidated, providing data to support its formulation development and regulatory filings .
    Denagliptin
  • HY-147858

    PROTACs EGFR Apoptosis Cancer
    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC EGFR degrader 7
  • HY-148764

    Apoptosis Cancer
    M47 is a small molecule that selectively destabilizes Cryptochrome 1 (CRY1) and increases degradation of the CRY1 in the nucleus. M47 enhances apoptosis in Ras-transformed P53-deficient mouse skin fibroblast lines and enhances life span in p53 knockout mice. M47 can be used in research of cancer .
    M47
  • HY-114312
    MD-224
    4 Publications Verification

    PROTACs MDM-2/p53 E1/E2/E3 Enzyme Cancer
    MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent . MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MD-224
  • HY-156084

    CDK PROTACs Apoptosis c-Myc Cancer
    LL-K9-3 is a potent small-molecule degrader of CDK9-cyclin T1. LL-K9-3 has anti-proliferative and pro-apoptotic activities and suppresses downstream signaling of CDK9 and AR. Moreover, LL-K9-3 inhibits AR and Myc-driven oncogenic transcriptional programs .
    LL-K9-3
  • 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 .
    PROTAC AR-NTD degrader 1
  • HY-149433

    Androgen Receptor Apoptosis Cancer
    BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .
    BWA-522
  • HY-10585G

    Dipropylacetic acid

    Organoid HDAC Autophagy Mitochondrial Metabolism HIV Notch Apoptosis Endogenous Metabolite Infection Neurological Disease Metabolic Disease Cancer
    Valproic acid (GMP) is Valproic acid (HY-10585) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Valproic acid (VPA) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM. Valproic acid inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches .
    Valproic acid
  • HY-120625

    HSP Cancer
    PU3 is a small molecule inhibitor of Hsp90 that competes with geldanamycin for Hsp90. PU3 induces degradation of proteins, including Her2, similar to geldanamycin. PU3 inhibits the growth of breast cancer cells, causing retinoblastoma protein hypophosphorylation, G1 arrest, and differentiation. PU3 represents a novel class of synthetic compounds that bind to Hsp90 and inhibit the proliferation of cancer cells. PU3 could provide a new strategy for the treatment of cancers .
    BMS-358233
  • HY-125001

    Others Others
    JH-VIII-49 is a potent and selective CDK8 inhibitor with excellent biological activity. The synthesis of JH-VIII-49 is simplified to eight steps with an overall yield of 33%, making it suitable for large-scale production. JH-VIII-49 promotes CDK8 inhibition through its steroid skeleton design. JH-VIII-49 provides a basis for the subsequent development of more complex bivalent small molecule degraders .
    JH-VIII-49
  • HY-103608

    VHL Ligand-Linker Conjugates 11; E3 ligase Ligand-Linker Conjugates 11

    E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
    (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl
  • HY-138111

    p-Nitopheyl β-D-cellotetaoside

    Fluorescent Dye Others
    4-Nitrophenyl β-D-cellotetraoside (p-Nitopheyl β-D-cellotetaoside) is a small molecule cellulose mimetic consisting of a tetramer of D-glucose units linked by β-1-4 glycosidic bonds. The fragmentation pattern of 4-Nitrophenyl β-D-cellotetraoside after enzymatic hydrolysis can be analyzed by TLC or by the release of 4-nitrophenol, which has a strong absorbance at 395 nm in alkaline solutions. 4-Nitrophenyl β-D-cellotetraoside can be used in cellulose degradation studies to determine the specificity of cellulases .
    4-Nitrophenyl β-D-cellotetraoside
  • HY-129265

    Polo-like Kinase (PLK) Cancer
    Poloxin-2 is a small molecule Plk1 PBD inhibitor that can effectively induce cell mitotic arrest with an EC50 of approximately 15 μM in HeLa cells. Poloxin-2HT was developed by conjugating a hydrophobic tag (HT) to Poloxin-2, a new application of inhibitors targeting protein-protein interactions. Poloxin-2HT significantly enhanced the effects on cell viability and apoptosis by selectively degrading Plk1 protein, and its effect was stronger than that of untagged Poloxin-2. These data validate hydrophobic tags as a new strategy for targeting and disrupting disease-associated proteins.
    Poloxin-2
  • HY-117051

    Others Cancer
    STA-2842 is a small molecule agent that inhibits heat shock protein 90 (HSP90) to treat autosomal dominant polycystic kidney disease (ADPKD). The disease is caused by inherited mutations in the PKD1 or PKD2 genes that aberrantly activate multiple signaling proteins and pathways that regulate cell proliferation. Through network construction, we found that many HSP90 client proteins associated with ADPKD are regulated by HSP90. STA-2842 induced degradation of these clients in Pkd1?/? primary kidney cells and in vivo. In experiments using conditional Cre-mediated in vivo knockout of Pkd1 in mice, we found that weekly administration of STA-2842 for 10 weeks significantly reduced initial renal cyst formation and kidney growth in mice and slowed disease progression in mice with pre-existing cysts. These improved disease phenotypes were accompanied by improvements in renal function markers and reductions in the expression and activity of HSP90 clients and their effectors, with the extent of this inhibition correlating with the extent of cyst expansion in individual animals. Pharmacokinetic analysis showed that HSP90 was overexpressed in cystic kidney tissue and HSP90 inhibitors were selectively retained in cystic tissue, which is similar to the situation in solid tumors. These results provide a preliminary basis for evaluating HSP90 inhibitors as therapeutic agents for ADPKD.
    STA-2842

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