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protein folding activity

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27

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Biochemical Assay Reagents

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Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15435
    CHAPS
    4 Publications Verification

    		 Exosomes Biochemical Assay Reagents Others
    CHAPS is a cholic acid-derived, sulfobetaine-type zwitterionic detergent and micelle-forming agent. CHAPS exhibits properties of weak cationic or nonionic surfactants in different solution systems, undergoes micellization, and forms small, loose hydrophilic aggregates that are temperature-dependent. CHAPS stabilizes mononucleosomes under different ionic strengths, reduces nucleosome sequence specificity, promotes sliding of histone cores along DNA, solubilizes Tamm-Horsfall protein to reduce its interference with urinary exosome isolation, and maintains vesicle structure and the activity of related proteins at the same time. CHAPS is used to recover native folded fusion proteins, enhance the binding capacity of GST fusion proteins, and restore GST enzyme activity. However, CHAPS cannot refold proteins denatured by urea, guanidine hydrochloride or heat, nor can it construct the structure of intrinsically disordered proteins. CHAPS is commonly used in research on the separation and purification of membrane proteins .
    CHAPS
  • HY-15346
    Copanlisib
    Maximum Cited Publications
    34 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
    34 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-15589
    GW9508
    5+ Cited Publications

    		 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-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-18705
    Azoramide
    5+ Cited Publications

    		 Apoptosis Reactive Oxygen Species (ROS) 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+ Cited Publications

    		 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-19369
    L-685458
    5+ Cited Publications

    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-15435A
    CHAPS hydrate
    4 Publications Verification

    		 Biochemical Assay Reagents Exosomes Others
    CHAPS hydrate is a cholic acid-derived, sulfobetaine-type zwitterionic detergent and micelle-forming agent. CHAPS hydrate exhibits properties of weak cationic or nonionic surfactants in different solution systems, undergoes micellization, and forms small, loose hydrophilic aggregates that are temperature-dependent. CHAPS hydrate stabilizes mononucleosomes under different ionic strengths, reduces nucleosome sequence specificity, promotes sliding of histone cores along DNA, solubilizes Tamm‑Horsfall protein to reduce its interference with urinary exosome isolation, and maintains vesicle structure and the activity of related proteins at the same time. CHAPS hydrate is used to recover native folded fusion proteins, enhance the binding capacity of GST fusion proteins, and restore GST enzyme activity. However, CHAPS hydrate cannot refold proteins denatured by urea, guanidine hydrochloride or heat, nor can it construct the structure of intrinsically disordered proteins. CHAPS hydrate is commonly used in research on the separation and purification of membrane proteins .
    CHAPS hydrate
  • 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-178155
    AP232

    		DNA/RNA Synthesis Autophagy Cancer
    AP232 is a selective U2AF1-UHM Inhibitor with an IC50 of 7.96 μM. AP232 exhibits 2.8-24-fold selectivity against other UHM-containing proteins. AP232 exerts anti-leukemia activity and shows higher activities in cell lines carrying splicing factor mutations. AP232 can induce leukemia cells G2/M and G1 arrest, impair lysosome acidification, and inhibit autophagy. AP232 can be used for the research of cancer, such as Leukemia .
    AP232
  • 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, affects the homeostasis, folding and assembly processes of viral proteins, and reduces the replication capacity of viruses. Pochonin D reduces the infiltration of inflammatory cells, decreases the secretion of inflammatory cytokines such as TNF-α and IL-1β, and alleviates inflammatory responses. Pochonin D is a promising candidate for research on human rhinovirus (HRV) infection and cancer .
    Pochonin D
  • 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-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-178155A
    AP232 dihydrochloride

    		DNA/RNA Synthesis Autophagy Cancer
    AP232 dihydrochloride is a selective U2AF1-UHM Inhibitor with an IC50 of 7.96 μM. AP232 dihydrochloride exhibits 2.8-24-fold selectivity against other UHM-containing proteins. AP232 dihydrochloride exerts anti-leukemia activity and shows higher activities in cell lines carrying splicing factor mutations. AP232 dihydrochloride can induce leukemia cells G2/M and G1 arrest, impair lysosome acidification, and inhibit autophagy. AP232 dihydrochloride can be used for the research of cancer, such as Leukemia .
    AP232 dihydrochloride
  • HY-15589R
    GW9508 (Standard)

    		Free Fatty Acid Receptor Potassium Channel Reference Standards Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    GW9508 (Standard) is the analytical standard of GW9508. This product is intended for research and analytical applications. 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 (Standard)
  • HY-176271
    MAO-B-IN-45

    		Ferroptosis Monoamine Oxidase Glutathione Peroxidase Reactive Oxygen Species (ROS) Tau Protein Amyloid-β Neurological Disease
    MAO-B-IN-45 is a dual inhibitor of ferroptosis and MAO-B. MAO-B-IN-45 shows selectivity towards MAO-B with an IC50 of 87.47 nM and selectivity exceeding 229-fold for MAO-B over MAO-A. MAO-B-IN-45 has excellent antiferroptosis activity through modulation of the iron metabolic pathway and GSH-GPX4 axis in vitro. MAO-B-IN-45 improves cognitive and behavioral impairments in 3×Tg (APP/Tau/Ps1) AD mouse and significantly reduced the levels of ferritin heavy chain 1 (FTH1), APP, and Tau phosphorylation (p-Tau) proteins in the brain.
    MAO-B-IN-45
  • 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-15346R
    Copanlisib (Standard)
    1 Publications Verification

    BAY 80-6946 (Standard)

    		 Reference Standards 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-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-155232
    PI3Kδ-IN-16

    		PI3K Apoptosis Cancer
    PI3Kδ-IN-16 is a potent and selective PI3Kδ inhibitor with an IC50 value of 0.9 nM. PI3Kδ-IN-16 has a strong anti-proliferative effect on SU-DHL-6 cells, causing cell cycle arrest and inducing apoptosis. PI3Kδ-IN-16 tightly bins to PI3Kδ protein with a planar-shaped conformation. The kinase activity of PI3Kδ-IN-16 which is ~378-fold over PI3Kα, 412-fold over PI3Kβ, and 10-fold over PI3Kγ. PI3Kδ-IN-16 can be used for the study of hematologic malignancies .
    PI3Kδ-IN-16
  • 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-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-174430
    WWQ-131

    		Ligands for Target Protein for PROTAC JAK Cancer
    WWQ-131 is a potent selective JAK2 inhibitor with an IC50 of 2.56 nM. WWQ-131 shows >252-fold selectivity over JAK1, JAK3, and TYK2. WWQ-131 exhibits antiproliferative activity against cancer cells. WWQ-131 is the ligand for target protein for PROTAC JAK2 degrader-1 (HY-174428). WWQ-131 can be used for the research of myeloproliferative neoplasms (MPNs) .
    WWQ-131
  • 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-179623
    PI3Kα-IN-29

    		PI3K mTOR Akt CDK Cadherin Cancer
    PI3Kα-IN-29 is a potent, orally active and selective PI3Kα with an IC50 of 2.5 nM. PI3Kα-IN-29 exhibits >400-fold selectivity over PI3Kβ/δ/γ/mTOR. PI3Kα-IN-29 selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses PI3K/AKT/mTOR signaling, induces G1 arrest, and inhibits migration. PI3Kα-IN-29 inhibits tumor growth in a T47 mouse model. PI3Kα-IN-29 can be used for the research of breast cancer .
    PI3Kα-IN-29

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