Otros inhibidores

<p>cn-716 is a novel Zika virus (ZIKV) NS2B-NS3pro protease inhibitor.</p>

<p>Galactostatin is an inhibitor of β-galactosidase.</p>

<p>KF 20274 is an adenosine A1 antagonist; purinergic receptor antagonist.</p>

<p>EBOV-GP-IN-1 (Compound 28) is a potent inhibitor of Ebola entry, acting on the Ebola virus envelope glycoprotein (EBOV-GP) (IC50: 0.05 μM).</p>

<p>(S)-5-hydroxy-6-methoxy Duloxetine, an active metabolite of the (S)-duloxetine, functions as a serotonin (5-HT) and norepinephrine reuptake inhibitor.</p>

<p>Epicochlioquinone A inhibits rat liver microsomal ACAT with an IC50 of 1.7 μM and inhibits plasma lecithin-cholesterol acyltransferase (LCAT) with an IC50 of 15.8 μM. At a dosage of 75 mg/kg, it can reduce cholesterol absorption in rats by 50%.</p>

<p>Carzinophillin A exhibits inhibitory effects on both ascites carcinoma and Yoshida sarcoma.</p>

<p>Nolpitantium is a potent, selective NK1 receptor antagonist that inhibits substance P without affecting NK2/NK3 receptors.</p>

<p>Mutalomycin is a polyether antibiotic with activity against Gram-positive bacteria, mycoplasma, and coccidia.</p>

<p>5-Hydroxymethylblasticidin S is a broad-spectrum antibiotic found in Streptomyces setonii.</p>

<p>FR 900452 is a platelet activating factor antagonist from fermentatiion products of Streptomyces phaeofaciens.</p>

<p>Cetoniacytone B inhibits the growth of HEPG2 and MCF7 human tumor cell lines, with a GI50 of 4.4 μM.</p>

<p>OPN expression inhibitor 1 is an osteopontin expression inhibitor used in the study of breast cancer metastasis.</p>

<p>(S)-Butaprost (free acid) is a potent and highly selective EP2 receptor agonist[1].</p>

<p>SK&amp;F 108361 is a symmetric diol that binds HIV-1 protease symmetrically.</p>

<p>Lunacalcipol is used for the treatment of Secondary Hyperparathyroidism.</p>

<p>Trk-IN-8: TRK inhibitor with IC50 of 0.42 nM (TRKA), 0.89 nM (TRKA-G595R), 1.5 nM (TRKC-G623R).</p>

<p>MK-7128 is a CB1 receptor inverse agonist.</p>

<p>PARP10/15-IN-1 (compound 8l) is a dual PARP10 and PARP15 inhibitor with IC50s of 160 nM and 370 nM, respectively. It can be used in cancer research[1].</p>

<p>AFM-30a hydrochloride: selective PAD2 inhibitor, EC50 9.5 μM; blocks H3 guanylation, EC50 0.4 μM; used for cancer and autoimmune research.</p>

<p>S39625 is a stable, potent topoisomerase I inhibitor with anticancer properties, resistant to efflux transporters, inducing gamma-H2AX at nanomolar levels.</p>

<p>Cirramycin B1 exhibits activity against both Gram-positive bacteria, Gram-negative bacteria, and mycoplasmas.</p>

<p>Antibacterial agent 69 is a novel structural antimicrobial modulator that can be used against lethal multidrug-resistant bacterial infections (MIC: 2.978 μM).</p>

<p>Pamiparib (BGB-290) is a selective PARP inhibitor that blocks DNA repair and promotes apoptosis.</p>

<p>Cytosaminomycin B exhibits activity against Eimeria Tenella coccidia.</p>

<p>Potent P-gp inhibitor 2 reverses Doxorubicin resistance in colorectal carcinoma cells with IC50 of 0.22 µM.</p>

<p>Cuevaene B can be isolated from the Streptomyces genus gdmAI-disrupted LZ35 strain. This compound exhibits moderate activity against Gram-positive bacteria, such as Bacillus subtilis (strain ATCC 11060), and shows moderate activity against fungi, including Fusarium verticillioides (strain S68) and Rhizoctonia solani (strain GXE4).</p>

<p>PD-1/PD-L1-IN-30: Cancer research inhibitor with 0.018 μM IC50.</p>

<p>Cuevaene A can be isolated from the Streptomyces genus gdmAI-disrupted LZ35 strain. It exhibits moderate activity against Gram-positive bacteria, such as Bacillus subtilis (strain ATCC 11060), and demonstrates moderate activity against fungi, including Fusarium verticillioides (strain S68) and Rhizoctonia solani (strain GXE4).</p>

<p>YKL-04-085 inhibits viral translation effectively, with strong antiviral action at much lower doses than those affecting host-cell growth.</p>

<p>IACS-8779 is a potent STING agonist that efficiently stimulates interferon gene activity and exhibits strong systemic antitumor effects.</p>

<p>Pyralomicin 2c is an antibiotic with antibacterial properties.</p>

<p>Enprostil: synthetic PGE2 analog, reduces gastric acid, protects mucosa, lowers post-meal gastrin, treats ulcers effectively and safely.</p>

<p>Carpetimycin B exhibits potent activity against both Gram-positive and Gram-negative bacteria, including those that produce β-lactamase. Carpetimycin B is also a strong inhibitor of β-lactamase (β-lactamase).</p>

<p>YW3-56: PAD2 &amp; PAD4 inhibitor (IC50 = 0.5-5 μM), halts U2OS cell growth (IC50 ~2.5 μM), reduces S-180 &amp; MDA-MB-231 tumor growth in mice.</p>

<p>Iloprost, a potent prostacyclin analog, binds IP &amp; EP1 receptors (Ki 11 nM), contains 16(S/R) isomers, and inhibits platelets (IC50 65 nM).</p>

<p>Cenicriviroc Sulfone, a Cenicriviroc derivative, inhibits CCR2/CCR5 to block HIV entry into cells.</p>

<p>Dinordrin is an implantation inhibitor and hormone.</p>

<p>Thiazolo[5,4-c]pyridin-4(5H)-one is a compound used for diagnostic imaging of TDP-43, in PET imaging of neurodegenerative diseases ALS、AD、FTD、LATE.</p>

<p>MK-8970 is an acetal carbonate prodrug of raltegravir with enhanced colonic absorption.</p>

<p>Bacithrocin C is a thrombin inhibitor that suppresses the activity of thrombin, factor Xa, trypsin, and papain, with IC50 values of 80 μM, 15 μM, 1.3 μM, and 0.02 μM, respectively.</p>

<p>Vindeburnol is a cerebral vasodilator vincamine analog that bears neuroprotective properties.</p>

<p>ALK5-IN-82 is a potent and selective inhibitor of activin receptor-like kinase 5 (ALK5), demonstrating an IC50 value of 9.1 nM. This compound effectively suppresses the expression of α-smooth muscle actin (α-SMA), collagen I, and the proteinases tissue inhibitor of metalloproteinase 1 (TIMP-1) and matrix metalloproteinase 13 (MMP-13) in human umbilical vein endothelial cells induced by transforming growth factor-β. ALK5-IN-82 shows potential for use in research related to cardiac fibrosis.</p>

<p>Epicorazine B exhibits activity against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE), with a minimum inhibitory concentration (MIC) of 12.5-25 μg/mL. It is also effective against Candida albicans, with an MIC of 25 μg/mL.</p>

<p>BI-1388 is a potent HCV NS3 protease inhibitor; halts replication across genotypes, including D168V/R155K mutants.</p>

<p>FTI 276 TFA targets plasmodium falciparum &amp; humans, inhibits PFT with IC50s: 0.9 nM (parasite) &amp; 0.5 nM (human).</p>

<p>Naltalimide: µ-opioid receptor partial agonist, improves bladder storage by affecting spinal cord reflex.</p>

<p>3-O-Demethylmonensin A is a polyether antibiotic produced by Streptomyces cinnamonensis (strain LO-63).</p>

<p>Arterolane, an adenosine triphosphatase inhibitor, is used potentially for the treatment of malaria.</p>

<p>Reumycin is a 7-azaindole antibiotic that exhibits cytotoxicity against tumor cells such as Ellrich carcinoma, Sarcoma-180, Sarcoma-37, and lymphosarcoma.</p>

<p>Compound R-13, a potent inhibitor of hCA I/II/IV/IX with K i s of 60.7, 320.7, 2298, and 35.2 nM.</p>

<p>Curvulic acid exhibits relatively weak activity against both Gram-positive and Gram-negative bacteria.</p>

<p>Deoxyfrenolicin is a quinone antibiotic that can be isolated from the fermentation broth of the Streptomyces roseofulvus strain AM-3867 and belongs to the frenolicin class of antibiotics. This compound exhibits in vitro antibacterial activity and is effective in inhibiting the activity of Mycoplasma gallisepticum.</p>

<p>Epoxyquinomicin C is an antibiotic that can be isolated from Amycolatopsis sp. It exhibits anti-inflammatory properties against collagen-induced arthritis and is also utilized in the synthesis of the NF-κB inhibitor DHMEQ.</p>

<p>THU dihydrate, a potent CDA inhibitor, outperforms cytidine by blocking the enzyme's active site.</p>

<p>PARP1-IN-5 is a potent, selective, orally active, low-toxicity PARP-1 inhibitor with an IC50 value of 14.7 nM. PARP1-IN-5 can be used in cancer research.</p>

<p>Cephemimycin exhibits mild antibacterial and antifungal activity.</p>

<p>Croconic acid (disodium) (Nacr) enhances gene expression related to lysine crotonylation (Kcr) modification, which promotes cell growth and proliferation. This compound also shows promise in boosting somatic cell nuclear transfer (SCNT) efficiency and optimizing research in cell culture conditions.</p>

<p>DS88790512, IC50 at 11 nM, is an effective, selective, oral bioeffective TRPC6 inhibitor.</p>

<p>SARS-CoV-2-IN-6 is an inhibitor of SARS-CoV-2 3CLpro with the IC 50 value of 73 nM.</p>

<p>Dup-714 is a thrombin inhibitor.</p>

<p>TSWV-IN-1 is an anti-TSWV drug with potential TSWV N.</p>

ABL-001-Amide-PEG3-acid, an analogue to ABL-001, primarily serves as a labeled chemical or fluorescent probe.

<p>Sdz 210-096: a 14 beta-benzyl morphinan, mu/kappa opiate receptor antagonist, stimulates LH secretion in rats.</p>

<p>Chelocardin exhibits activity against Gram-positive and Gram-negative bacteria.</p>

<p>6"'-Deamino-6"'-hydroxyneomycin B is an aminoglycoside antibiotic produced by [Streptomyces fradiaeUC 75]. It is effective against both Gram-positive and Gram-negative bacteria and serves as an intermediate in the biosynthesis of neomycin.</p>

<p>SARS-CoV-2-IN-22 is a SARS-CoV-2 pseudovirus inhibitor (IC50: 16.96 μM).</p>

<p>Glyphosate-trimesium is a herbicide.</p>

<p>L 739749 is a CAAX peptidomimetic. It is also an inhibitor of farnesyl-protein transferase.</p>

<p>BMS-554417 inhibits IGF-IR/insulin receptors, curbing cell proliferation and tumor growth, with IC50 values of 120 nm–&gt;8.5 μmol/L.</p>

<p>Chitinovorin A is a β-lactam antibiotic (antibiotic) that exhibits weak inhibitory activity against Gram-negative bacteria.</p>

<p>Retelliptine, a DNA topoisomerase II inhibitor, is used potentially for the treatment of cancer.</p>

<p>Flavipucine (Flavipucin) is a glutarimide antibiotic found in the Aspergillus flavipes F-2090/7 strain. It exhibits antibacterial activity against Bacillus subtilis, possesses antiprotozoal properties, and demonstrates cytotoxic effects on various cancer cells.</p>

<p>3-O-Demethyl-2'-N-glylfortimicin B is a type of aminoglycoside antibiotic.</p>

<p>Rafutrombopag is a thrombopoietin (TPO) agonist.</p>

<p>Jietacin A exhibits nematocidal activity, capable of killing Burs helenchus Lignicolus at a concentration of 0.25 μg/mL.</p>

<p>SphK2-IN-2 (21g) is a potent and selective inhibitor of SphK2 (IC50: 0.23 μM).</p>

<p>Coriolin B exhibits activity against Gram-positive bacteria, weak activity against Gram-negative bacteria, yeast, and Trichomonas vaginalis. At a concentration of 5 μg/mL, Coriolin B inhibits 61.6% of Yoshida sarcoma growth but shows no inhibitory effect on Ehrlich ascites carcinoma in animals.</p>

<p>Kynapcin-28 is a non-competitive inhibitor of prolyl endopeptidase (PEP) with an IC50 of 76.80 μM and exhibits weak inhibitory effects on other serine proteases.</p>

<p>AZD-3199 dihydrobromide is a β2 adrenergic receptor agonist potentially for the treatment of asthma and chronic obstructive.</p>

<p>DSP-6952 is a 5-HT4 receptor partial agonist, inhibiting visceral hypersensitivity and ameliorating gastrointestinal dysfunction.</p>

<p>Basroparib is an inhibitor of ribose polymerase (PARP) and has shown antitumour effects.</p>

<p>GR-112000 is a peptide-based tachykinin NK2 receptor antagonist.</p>

<p>Antitumor agent-51 targets osteosarcoma with 21.9 nM IC50, high selectivity, and low toxicity.</p>

<p>Deoxyradicinin is a biosynthetic precursor of Radicinin. It can inhibit Xylella fastidiosa and Liberibacter crescens, with a minimum inhibitory concentration (MIC) of 3.5 μg/mL against Liberibacter crescens. Deoxyradicinin is applicable for research on controlling plant diseases caused by these pathogens.</p>

<p>Cremeomycin exhibits activity against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), with a minimum inhibitory concentration (MIC) of 0.2-0.39 μg/mL. It also demonstrates cytotoxic effects in vitro against mouse tumor cell lines P388, L1210, IMC, S180, B16, and SS3.</p>

<p>Keap1-Nrf2-IN-1 TFA (compound35) is a potent inhibitor (IC50: 43 nM) protecting against acetaminophen liver damage.</p>

<p>Mimosine, a plant amino acid, is known to act as a normoxic inducer of hypoxia-inducible factor (HIF).</p>

<p>5-HT1A antagonist; Ki=8nM, Kb=0.04nM. PDE4B IC50=80.4μM; PDE7A IC50=151.3μM. Good biofilm penetration, stable, anticognitive, antidepressant.</p>

<p>PI3K-IN-27 is a potent PI3K inhibitor, relevant for cancer and immune disease research. See patent WO2021233227A1.</p>

<p>AD5075 is a bioactive chemical.</p>

<p>ROS1-IN-1, a potent ROS1 kinase inhibitor, has an IC50 of 0.097 μM.</p>

<p>Clecarmycin C is an antitumor antibiotic that demonstrates cytotoxic and antitumor properties. Additionally, Clecarmycin C exhibits antibacterial activity.</p>

<p>GPX-100, a non-cardiotoxic doxorubicin analog, intercalates DNA and inhibits replication, repair, and protein synthesis.</p>

<p>Pradimicin T2 is an antibiotic with activity against filamentous fungi and yeast-like fungi.</p>

<p>β-Carotene-15,15ʹ-epoxide acts as an XIAP antagonist with pro-apoptotic (Apoptosis) and anti-tumor properties, found in the leaves of Spondias mombin. In rat models of DMBA-induced breast cancer, it induces tumor cell apoptosis by binding to the BIR3 domain of the XIAP protein, thereby inhibiting its interaction with caspase-9. Additionally, β-carotene-15,15ʹ-epoxide significantly reduces BCL-2, COX-2, and TNF-α expression in tumor tissue, decreases MDA levels, enhances catalase activity, and modulates biochemical markers in serum such as LDH, ALP, and ALT, indicating its antioxidant, anti-inflammatory, and metabolic protective effects. This compound is useful for researching inflammation-related diseases and tumors such as breast cancer.</p>

<p>3-Methoxy-2,5-toluquinone is an antimicrobial agent that exhibits moderate antibacterial and antifungal properties.</p>

<p>Saframycin A exhibits antibacterial activity against Gram-positive bacteria and shows weaker effects on Gram-negative bacteria and mycobacteria. Additionally, it inhibits mouse lymphocyte L-1210 cells, with an ID50 of 0.0056 μM.</p>

<p>9-O-Demethyltrigonostemone is a natural IDO1 inhibitor, cytotoxic and antiplasmodial agent from the Roots of Strophioblachia fimbricalyx.</p>

<p>Chuangxinmycin is an antibiotic that can be isolated from Actinoplanes tsinanensis CPCC 200056. It exhibits antibacterial activity both in vitro and in vivo, making it useful for research related to infections.</p>

<p>Dexnebivolol (R67138), a ß-adrenergic antagonist, is Nebivolol's enantiomer with β1 blocking and vasodilation properties.</p>

<p>1,6-Dihydroxy-2-chlorophenazine exhibits weak antifungal and anti-yeast activity.</p>

<p>4-Nitrochalcone (2-(4-Nitrobenzylidene)acetophenone) inhibits proteasomes and suppresses TNFα-induced NF-κB activity.</p>

<p>5-HT1A/5-HT7 antagonist; 5-HT1A Ki=8 nM, 5-HT7 Ki=451 nM; PDE4B IC50=80.4 μM, PDE7A IC50=151.3 μM; stronger than escitalopram.</p>

<p>NAZ2329: Cell-permeable, targets R5 RPTPs, inhibits hPTPRZ1 (IC50=7.5 μM) &amp; hPTPRG (IC50=4.8 μM), hampers glioblastoma growth, affects stem cell traits.</p>

<p>PARP7-IN-12, a potent inhibitor targeting PARP7, exhibits an IC50 of 7.836 nM. This compound is applicable in cancer research.</p>