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Results for "

protein folding activity

" in MedChemExpress (MCE) Product Catalog:

20

Inhibitors & Agonists

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12019
    SGX-523
    5+ Cited Publications

    		 c-Met/HGFR Cancer
    SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity .
    SGX-523
  • HY-15652
    Freselestat

    ONO-6818; ONO-PO-736

    		 Elastase Inflammation/Immunology
    Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .
    Freselestat
  • HY-124652
    TBK1/IKKε-IN-4

    		IKK Cancer
    TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR .
    TBK1/IKKε-IN-4
  • HY-18705
    Azoramide
    5 Publications Verification

    		 Apoptosis Reactive Oxygen Species Caspase Bcl-2 Family Mitochondrial Metabolism Endocrinology
    Azoramide is a potent, orally active small-molecule modulator of the unfolded protein response (UPR). Azoramide improves ER protein folding and elevates ER chaperone capacity, which together protects cells against ER stress. Azoramide alleviates PLA2G6 mutant-induced ER stress through modulating unfolded protein response, and enhances the CERB signaling to rescue mitochondrial function, thereby preventing apoptosis of DA neurons. Azoramide has antidiabetic activity .
    Azoramide
  • HY-18669
    ML346
    5 Publications Verification

    		 HSP Cancer
    ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity. ML346 induces specific increases in genes and protein effectors of the heat shock response (HSR), including chaperones such as Hsp70, Hsp40, and Hsp27 .
    ML346
  • HY-135189
    6-Aminophenanthridine

    		Others Others
    6-Aminophenanthridine inhibits the protein folding activity of the ribosome (PFAR). 6-Aminophenanthridine competitively occludes the protein substrates from binding to rRNA and thereby inhibits PFAR .
    6-Aminophenanthridine
  • HY-120159
    GS-493

    		SHP2 SHP1 Phosphatase Cancer
    GS-493 is a selective protein tyrosine phosphatase SHP2 (PTPN11) inhibitor with an IC50 of 71 nM. GS-493 is 29- and 45-fold more active toward SHP2 than related SHP1 and PTP1B. GS-493 blocks cellular motility and growth of cancer cells. Antitumor activity .
    GS-493
  • HY-15652A
    Freselestat quarterhydrate

    ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate

    		 Elastase Inflammation/Immunology
    Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity .
    Freselestat quarterhydrate
  • HY-116919
    MLS000536924

    		Lipoxygenase Cardiovascular Disease
    MLS000536924 is a potent and selective inhibitor of human epithelial 15-lipoxygenase-2 with competitive activity. MLS000536924 exhibits more than 50-fold selectivity in inhibiting h15-LOX-2 and can be effectively applied to study its role in atherosclerosis, cystic fibrosis, and ferroptosis. The binding mode of MLS000536924 shows stronger restriction of protein movement than other inhibitors, further verifying its higher biological activity .
    MLS000536924
  • HY-134561
    6-Amino-8-trifluoromethylphenanthridine

    6A-8tFP

    		 Prion Protein Infection
    6-Amino-8-trifluoromethylphenanthridine (6A-8tFP) is an antiprion agent and a derivative of 6-aminophenanthridine (HY-135189). It inhibits protein folding activity of the ribosome (PFAR) when used at a concentration of 150 μM.2 6A-8tFP directly competes with protein substrates for the ribosomal active site.
    6-Amino-8-trifluoromethylphenanthridine
  • HY-15589
    GW9508
    5 Publications Verification

    		 Free Fatty Acid Receptor Potassium Channel Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .
    GW9508
  • HY-15346
    Copanlisib
    Maximum Cited Publications
    26 Publications Verification

    BAY 80-6946

    		 PI3K Apoptosis Cancer
    Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
    Copanlisib
  • HY-15346A
    Copanlisib dihydrochloride
    Maximum Cited Publications
    26 Publications Verification

    BAY 80-6946 dihydrochloride

    		 PI3K Apoptosis Cancer
    Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity .
    Copanlisib dihydrochloride
  • HY-N8353
    Stachybotramide

    		Others Metabolic Disease
    Stachybotramide is a natural fungal metabolite with the property of modulating the activity of cholesteryl ester transfer protein (CETP). Stachybotramide stimulates the transfer of cholesteryl esters (CE) from high-density lipoprotein (HDL) to very-low-density lipoprotein (VLDL) and low-density lipoprotein (LDL), increasing the transfer efficiency by 1.3- to 1.5-fold. Stachybotramide slightly reduced the transfer of cholesteryl esters from LDL and VLDL to HDL at 0.5 mM. The effect of Stachybotramide on the transfer of triglycerides (TG) from HDL was not significant. By these results, Stachybotramide was shown to preferentially stimulate the CETP-mediated transfer of cholesteryl esters from HDL to VLDL and LDL .
    Stachybotramide
  • HY-N14780
    Pochonin D

    (+)-Pochonin D

    		 HSP Interleukin Related Enterovirus Infection Inflammation/Immunology Cancer
    Pochonin D ((+)-Pochonin D) is an inhibitor of heat shock protein 90 (Hsp90) with antiviral and anti-inflammatory activities. Pochonin D inhibits Hsp90, affecting the homeostasis, folding, and assembly processes of viral proteins, reducing the replication ability of the virus. Pochonin D reduces the infiltration of inflammatory cells and the secretion of inflammatory cytokines such as TNF-α and IL-1β, alleviating the inflammatory response. Pochonin D is promising for research of Human rhinoviruses (HRV) infections and cancers .
    Pochonin D
  • HY-19369
    L-685458
    5 Publications Verification

    L-685,458

    		 γ-secretase Apoptosis Neurological Disease Cancer
    L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers .
    L-685458
  • HY-15346R
    Copanlisib (Standard)

    		PI3K Apoptosis Cancer
    Copanlisib (Standard) is the analytical standard of Copanlisib. This product is intended for research and analytical applications. Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
    Copanlisib (Standard)
  • HY-116748
    (±)-trans-1,2-Bis(2-mercaptoacetamido)cyclohexane

    		PDI Phosphatase
    (±)-trans-1,2-Bis(2-mercaptoacetamido)cyclohexane is a small-molecule dithiol catalyst with a low thiol pKa value (8.3) and high reduction potential (-0.24 V), capable of mimicking PDI activity. It catalyzes the activation of scrambled ribonuclease A (scrambled ribonuclease A) and promotes the formation of native disulfide bonds, thereby significantly enhancing protein folding efficiency. Adding (±)-trans-1,2-Bis(2-mercaptoacetamido)cyclohexane to the culture medium of Saccharomyces cerevisiae can increase the secretion of exogenously expressed Schizosaccharomyces pombe acid phosphatase by more than threefold. (±)-trans-1,2-Bis(2-mercaptoacetamido)cyclohexane holds great potential for applications in protein production and secretion research .
    (±)-trans-1,2-Bis(2-mercaptoacetamido)cyclohexane
  • HY-149760
    PVD-06

    		PROTACs Phosphatase Cancer
    PVD-06 is a selective PROTAC-class PTPN2 degrader (PTPN2/PTP1B selectivity index >60-fold) with anticancer activity. PVD-06 induces PTPN2 degradation via ubiquitination and proteasome-dependent pathways. PVD-06 can promote T cell activation and amplify IFN-γ-mediated cytotoxicity . PVD-06 consists of a target protein ligand (red part) PTPN2 ligand 1 (HY-168691), a PROTAC linker (black part) 6-Aminocaproic acid (HY-B0236), and an E3 ubiquitin ligase ligand (blue part) (S,R,S)-AHPC-Me (HY-112078). E3 ubiquitin ligase+linker can form 6-Aminocaproic acid-(S,R,S)-AHPC-Me (HY-168690).
    PVD-06
  • HY-170824
    SMD-3236

    		PROTACs Epigenetic Reader Domain Cancer
    SMD-3236 is a SMARCA2-targeted PRAOTAC degrader designed based on SMARCA ligands and VHL-1 ligands, with long-lasting antitumor activity in vivo. SMARCA2 is a synthetic lethal target in SMARCA4-deficient cancer cells, and SMD-3236 has a 2000-fold selectivity for degradation of SMARCA2 over SMARCA4, with a DC50< 1 nM and a Dmax>95%. SMD-3236 can induce SMARCA2 loss in tumor tissues while retaining SMARCA4 protein, and inhibit tumor growth in the H838 smarca4-deficient human cancer xenograft model. SMD-3236 is composed of target protein ligand (red part) SMI-1074 (HY-170817), PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate (HY-170825), and E3 ligase ligand (blue part) SMARCA2 ligand-14 (HY-170826), of which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 159 (HY-170827) .
    SMD-3236

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