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Plasma Stability

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48

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3

Biochemical Assay Reagents

5

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2

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1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-41189
    Fmoc-Val-Cit-PAB-PNP

    		ADC Linker Cancer
    Fmoc-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Val-Cit-PAB-PNP has superior plasma stability comparable to that of non-cleavable linkers .
    Fmoc-Val-Cit-PAB-PNP
  • HY-107749
    ML 190

    		Opioid Receptor Neurological Disease
    ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC50 of 120 nM and an EC50 of 129 nM, respectively .
    ML 190
  • HY-150719
    AIMP2-DX2-IN-1

    		Others Cancer
    AIMP2-DX2-IN-1 (Compound 35) is a potent AIMP2-DX2 inhibitor with an IC50 of 0.1063 μM .
    AIMP2-DX2-IN-1
  • HY-P6053
    KK-103

    		Opioid Receptor Neurological Disease
    KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect .
    KK-103
  • HY-143255
    Enpp-1-IN-11

    		Phosphodiesterase (PDE) Cancer
    Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer .
    Enpp-1-IN-11
  • HY-13611
    Diflomotecan

    BN 80915

    		 Topoisomerase Cancer
    Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds .
    Diflomotecan
  • HY-163004
    Type II TRK inhibitor 2

    		Trk Receptor Cancer
    Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA G595R and Ba/F3-TRKA G667C cell proliferation (IC50: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .
    Type II TRK inhibitor 2
  • HY-150681
    SARS-CoV-2 nsp14-IN-2

    		SARS-CoV Infection
    SARS-CoV-2 nsp14-IN-2 is a potent SARS-CoV-2 Nsp14 methyltransferase inhibitor with an IC50 value of 0.093 µM. SARS-CoV-2 nsp14-IN-2 shows antiviral activity. SARS-CoV-2 nsp14-IN-2 shows plasma and liver S9 stability. SARS-CoV-2 nsp14-IN-2 has the potential for the research of COVID-19 .
    SARS-CoV-2 nsp14-IN-2
  • HY-159564
    iNOS/COX-2-IN-3

    		COX NO Synthase Inflammation/Immunology
    iNOS/COX-2-IN-3 (compound 7d) is a dual inhibitor of iNOS and COX-2, with potential anti-inflammatory activity against LPS (HY-D1056)-induced RAW 264.7 cells (IC50=3.48 μM). iNOS/COX-2-IN-3 has good plasma stability, oral activity and gastric safety, and its inhibitory activity on iNOS and COX-2 expression is 5.43-fold and 2.37-fold that of Indomethacin (HY-14397), respectively .
    iNOS/COX-2-IN-3
  • HY-163291
    AM4085

    		Bacterial Infection
    AM4085 is an orally active Antagonist for FmlH with an IC50 of 0.19 μM. AM4085 reveals metabolic stability in mouse liver microsomes and blood plasma .
    AM4085
  • HY-160031
    GLP-1R agonist 19

    		GLP Receptor Cardiovascular Disease
    GLP-1R agonist 19 (M3190) is a potent and selective GLP-1R agonist. GLP-1R agonist 19 has excellent plasma stability, liver microsomal stability, and low hERG toxicity .
    GLP-1R agonist 19
  • HY-156188
    AChE-IN-41

    		Others Others
    AChE-IN-41 (Compound 2) is a compound of the Galantamine Memantine hybrid. AChE-IN-41 has the inhibition ability of cholinesterase. AChE-IN-41 shows higher plasma stability and comparable microsomal stability in vitro, while showing lower half-life and faster clearance in vivo .
    AChE-IN-41
  • HY-100432
    LOC14
    2 Publications Verification

    		 PDI Neurological Disease Inflammation/Immunology
    LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding . LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
    LOC14
  • HY-145842
    Encephalitic alphavirus-IN-1

    		Virus Protease Infection Neurological Disease
    Encephalitic alphavirus-IN-1 has antiviral activity for VEEV and EEEV with EC50s of 0.24 μM and 0.16 μM, respectively. Encephalitic alphavirus-IN-1 has robust mouse plasma stability, and no obvious cytotoxicity .
    Encephalitic alphavirus-IN-1
  • HY-155047
    BDM91514

    		Bacterial Infection
    BDM91514 improves antibiotic potency through AcrB inhibition. BDM91514 prevents the growth of E. coliBW25113 (EC90: 8 μM) in the presence of 8 μg/mL Pyridomycin. BDM91514 has suitable plasma and microsomal stability .
    BDM91514
  • HY-126254
    BI-4924
    1 Publications Verification

    		 Phosphoglycerate Dehydrogenase (PHGDH) Cancer
    BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h .
    BI-4924
  • HY-153715
    NV-354

    Mitochondria modulator-1

    		 Biochemical Assay Reagents Metabolic Disease
    Mitochondria modulator-1 is a mitochondrial regulator that stimulates mitochondrial ATP production. Mitochondria modulator-1 has good oral bioavailability, blood-brain barrier permeability, and good plasma stability. Mitochondria modulator-1 has the potential to study mitochondrial diseases .
    NV-354
  • HY-155011
    MB076

    		Others Others
    MB076 is a novel heterocyclic triazole with improved plasma stability. MB076 inhibits seven different Class C Acinetobacter-derived cephalosporinases (ADCs) β-lactamase variants with Ki values ＜ 1 μM. MB076 acts synergistically in combination with multiple cephalosporins to restore pBCSK(−) susceptibility .
    MB076
  • HY-143458
    FAK PROTAC B5

    		FAK PROTACs Cancer
    FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion .
    FAK PROTAC B5
  • HY-163289
    TSLP binder-1

    		Others Inflammation/Immunology
    TSLP binder-1 (compound 46) is a bicyclic peptide, which binds to thymic stromal lymphopoietin (TSLP) at the site used by IL-7Rα subunit, shows high affinity for TSLP, with KD of 13 nM. TSLP binder-1 reveals good stability in rat plasma and rat lung S9 fraction .
    TSLP binder-1
  • HY-118147
    ML356

    		Others Cancer
    ML356 (Compound 16) is an inhibitor for fatty acid synthase (FAS), that inhibits the thioesterase domain of FAS (FAS TE) with an IC50 of 0.334 μM, and blocks the de novo palmitate synthesis in PC-3 cell with an IC50 of 20 μM. ML356 exhibits good membrane permeability, and good stability in human and mouse plasma .
    ML356
  • HY-117187
    Corr4A

    		CFTR Others
    Corr4A is a chemical corrector, which can be used for cystic fibrosis. Corr4A interacts directly with the cystic fibrosis transmembrane conductance regulator (CFTR) or affects indirectly its folding process. Corr4A increases the expression of CFTR ΔF508 on the cell surface, thereby improving its transport to the plasma membrane and increasing the stability of the rescued mutant protein .
    Corr4A
  • HY-147547
    SV5

    		Amyloid-β Neurological Disease
    SV5 is a potent anti-Alzheimer agent. SV5 can significantly protect SHSY-5Y cells against Aβ1-42-induced death. SV5 shows moderate antioxidant and good neuroprotective activities. SV5 shows the high stability in human plasma and the best pharmacological profile .
    SV5
  • HY-161247
    5-HT2A antagonist 2

    		5-HT Receptor Metabolic Disease
    5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 .
    5-HT2A antagonist 2
  • HY-163403
    VEGFR-2-IN-43

    		VEGFR Cardiovascular Disease Cancer
    VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research .
    VEGFR-2-IN-43
  • HY-143877
    NN-390

    		HDAC Cancer
    NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) .
    NN-390
  • HY-144771
    SARS-CoV-2-IN-14

    		SARS-CoV Infection
    SARS-CoV-2-IN-14 (compound 6) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.39 μM. SARS-CoV-2-IN-14 is a niclosamide analogue. SARS-CoV-2-IN-14 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
    SARS-CoV-2-IN-14
  • HY-144772
    SARS-CoV-2-IN-15

    		SARS-CoV Infection
    SARS-CoV-2-IN-15 (compound 11) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.49 μM. SARS-CoV-2-IN-15 is a niclosamide analogue. SARS-CoV-2-IN-15 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
    SARS-CoV-2-IN-15
  • HY-144770
    SARS-CoV-2-IN-13

    		SARS-CoV Infection
    SARS-CoV-2-IN-13 (compound 5) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.057 μM. SARS-CoV-2-IN-13 is a niclosamide analogue. SARS-CoV-2-IN-13 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
    SARS-CoV-2-IN-13
  • HY-128943
    MAC glucuronide phenol-linked SN-38

    		Drug-Linker Conjugates for ADC Cancer
    MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) agent linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.Albumin-coupled MAC glucosidol-linked SN-38 shows good stability in mouse plasma .
    MAC glucuronide phenol-linked SN-38
  • HY-158082
    TRITC-dextran, MW 4000

    Tetramethyl rhodamine isothiocyanate glucan, MW 4000

    		 Fluorescent Dye Others
    TRITC-dextran MW 4000 (Tetramethyl rhodamine isothiocyanate glucan, MW 4000) is a fluorescent dye, with the molecular weight of 4 kD. TRITC-dextran MW 4000 exhibits an excitation wavelength of 555 nm. TRITC-dextran MW 4000 is vessel penetrate, which could label blood plasma to visualize the vasculature. TRITC-dextran MW 4000 is utilized in drug delivery for the stability of TRITC over a wide pH range (i.e. pH 2–11) and resistance to photo-bleaching .
    TRITC-dextran, MW 4000
  • HY-158082A
    TRITC-dextran, MW 20000

    Tetramethyl rhodamine isothiocyanate glucan, MW 20000

    		 Fluorescent Dye Others
    TRITC-dextran, MW 20000 (Tetramethyl rhodamine isothiocyanate glucan, MW 20000) is a fluorescent dye, with the molecular weight of 20 kD. TRITC-dextran MW 20000 exhibits an excitation wavelength of 555 nm. TRITC-dextran MW 20000 is vessel penetrate, which could label blood plasma to visualize the vasculature. TRITC-dextran MW 20000 is utilized in drug delivery for the stability of TRITC over a wide pH range (i.e. pH 2–11) and resistance to photo-bleaching .
    TRITC-dextran, MW 20000
  • HY-158082B
    TRITC-dextran, MW 40000

    Tetramethyl rhodamine isothiocyanate glucan, MW 40000

    		 Fluorescent Dye Others
    TRITC-dextran, MW 40000 (Tetramethyl rhodamine isothiocyanate glucan, MW 40000) is a fluorescent dye, with the molecular weight of 40 kD. TRITC-dextran MW 40000 exhibits an excitation wavelength of 555 nm. TRITC-dextran MW 40000 is vessel penetrate, which could label blood plasma to visualize the vasculature. TRITC-dextran MW 40000 is utilized in drug delivery for the stability of TRITC over a wide pH range (i.e. pH 2–11) and resistance to photo-bleaching .
    TRITC-dextran, MW 40000
  • HY-161819
    TRK-IN-29

    		Trk Receptor Cancer
    TRK-IN-29 (Compound B31) is a second-generation TRK inhibitor (IC50: 9 nM, 0.6 nM, 18 nM, 5 nM, 6 nM for TRKA G595R, TRKA F589L, TRKA G667C, TRKA and TRKC respectively). TRK-IN-29 inhibits the phosphorylation of TRKA. TRK-IN-29 has good antiproliferative activities against NTRK fusion positive cells. TRK-IN-29 has exellent plasma stability and moderate pharmacokinetic properties .
    TRK-IN-29
  • HY-169064
    HIV-1 inhibitor-75

    		HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-75 is a human immunodeficiency virus 1 (HIV-1) inhibitor, with an EC50 value ranging from 0.0039 to 0.338 μM. The binding target of HIV-1 inhibitor-75 is reverse transcriptase, with an IC50 value of 0.055 μM. HIV-1 inhibitor-75 shows good in vitro metabolic stability, exhibiting moderate clearance rates and a longer half-life in human plasma and liver microsomes .
    HIV-1 inhibitor-75
  • HY-P2161
    TAK-683

    		Kisspeptin Receptor Cancer
    TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
    TAK-683
  • HY-P2161B
    TAK-683 acetate
    1 Publications Verification

    		 Kisspeptin Receptor Cancer
    TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
    TAK-683 acetate
  • HY-P2161A
    TAK-683 TFA

    		Kisspeptin Receptor Cancer
    TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
    TAK-683 TFA
  • HY-161823
    Anti-MRSA agent 13

    		Bacterial Infection
    Anti-MRSA agent 13 (Compound 9b) is an agent against methicillin-resistant Staphylococcus aureus (MRSA), exhibiting a minimum inhibitory concentration (MIC) of 0.5–2 μg/mL against clinically isolated MRSA strains. Anti-MRSA agent 13 possesses favorable biosafety, plasma tolerance stability, and a low tendency to develop resistance. Anti-MRSA agent 13 disrupts cell walls and membranes, reduces metabolic activity, causes oxidative damage, affects DNA function, and ultimately leads to MRSA death through multi-target synergies .
    Anti-MRSA agent 13
  • HY-160023
    D3S-001

    		Ras Cancer
    D3S-001 is an orally active inhibitor for KRAS. D3S-001 inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. D3S-001 exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
    D3S-001
  • HY-159563
    Mal-va-mac-SN38

    		Drug-Linker Conjugates for ADC Cancer
    Mal-va-mac-SN38 is a drug-linker conjugate for ADC. Mal-va-mac-SN38 contains a ADC cytotoxin SN-38 (HY-13704) and a linker (HY-126364). Mal-va-mac-SN38 can rapidly and covalently bind with endogenous albumin in vivo, resulting in the formation of HSA-va-mac-SN38. Mal-va-mac-SN38 demonstrates exceptional stability in human plasma, and has anti-tumor and anti-metastasis effect .
    Mal-va-mac-SN38
  • HY-163783
    CSNK2-IN-1

    		Casein Kinase Infection
    CSNK2-IN-1 is a potent and selective CSNK2 inhibitor with IC50 of 1.7 nM and 0.66 nM for CSNK2A1 and CSNK2A2, respectively. CSNK2-IN-1 has antiviral activity against beta-coronaviruses such as SARS-CoV-2 and MHV. CSNK2-IN-1 has good solubility, metabolic stability, and low cytotoxicity, but its plasma concentration in vivo decreases rapidly and is insufficient to achieve pharmacological effects. CSNK2-IN-1 can be used in the research of antiviral drug development .
    CSNK2-IN-1
  • HY-164477
    FL442

    		Androgen Receptor Cancer
    FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .
    FL442
  • HY-162963
    PPARδ agonist 11

    		PPAR Inflammation/Immunology
    PPARδ agonist 11 (Compound 11) is a selective agonist for PPARδ with an EC50 of 20 nM. PPARδ agonist 11 reduces the levels of nitrite oxide (NO), proinflammatory cytokines TNFα and IL-6 in LPS (HY-D1056)-stimulated RAW264.7 cell, and exhibits anti-inflammatory efficacy via NF-κB pathway. PPARδ agonist 11 exhibits good stability in human liver microsomes and plasma. PPARδ agonist 11 ameliorates Carrageenan (HY-125474)-induced foot edema, and exhibits good pharmacokinetic characteristics with an bioavailability of ca. 100% .
    PPARδ agonist 11
  • HY-161988
    Antimicrobial agent-34

    		Bacterial Infection Inflammation/Immunology
    Antimicrobial agent-34 (compound 4h) is an antibacterial agent (MIC = 1–4 μg/mL), with a clogP value of 9.14. Antimicrobial agent-34 has good plasma stability (HC50 of 131.1 μg/mL) and good membrane selectivity (HC50/MIC is 65.6), with rapid sterilization capability. Antimicrobial agent-34 destroys the integrity of bacterial cell membranes, induces an increase in intracellular reactive oxygen species, and leaks protein and DNA, ultimately leading to bacterial death. Antimicrobial agent-34 demonstrates significant in vivo antibacterial potency in a mouse sepsis model infected with Staphylococcus aureus ATCC43300 .
    Antimicrobial agent-34
  • HY-169059
    Ferroptosis-IN-12

    		Ferroptosis Inflammation/Immunology
    Ferroptosis-IN-12 (Cpd-A1) is a ferroptosis inhibitor. Ferroptosis-IN-12 exhibits effective ferroptosis inhibition in Erastin (HY-15763)-treated mouse tubular epithelial cells (mTECs) and improves kidney function, alleviates renal tubular damage, and reduces inflammation in a dose-dependent manner in acute kidney injury (AKI) mouse models induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). Ferroptosis-IN-12 demonstrates good plasma stability and high distribution in kidney tissues in pharmacokinetic studies in mice. Ferroptosis-IN-12 holds promise for research in the field of acute kidney injury (AKI) .
    Ferroptosis-IN-12
  • HY-N3980
    Guaiol

    Champacol; Guaiac alcohol

    		 Autophagy RAD51 Infection Cardiovascular Disease Inflammation/Immunology Cancer
    Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
    Guaiol
  • HY-N3980R
    Guaiol (Standard)

    		Autophagy RAD51 Infection Cardiovascular Disease Inflammation/Immunology Cancer
    Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
    Guaiol (Standard)

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