FASN-IN-6;化合物 FASN-IN-6FASN-IN-6 (2024/9/14)
簡(jiǎn)介:fasn-in-6 (compound 44), a potent fatty acid biosynthesis (fab) inhibitor, serves as an antibacterial agent, exhibiting minimum inhibitory concentrations (mics) of 1 μg/ml for s. aureus atcc 25923 and 4 μg/ml for e. faecalis atcc 29212 [1].
Antiparasitic agent-18;化合物 Antiparasitic agent-18Antiparasitic agent-18 (2024/9/14)
簡(jiǎn)介:antiparasitic agent-18 (compound 3a) exhibits potent and selective antiprotozoal activity, demonstrating effective inhibition of t. brucei (ec 50 =0.4 μm), t. cruzi (ec 50 =0.21 μm), and l. donovani (ec 50 =0.26 μm) [1].
SARS-CoV-2-IN-60;化合物 SARS-CoV-2-IN-60SARS-CoV-2-IN-60 (2024/9/14)
簡(jiǎn)介:sars-cov-2-in-60 (compound 5a) is a specific, irreversible inhibitor of sars-cov-2 nsp16-nsp10 methyltransferase, competing with s-adenosylmethionine (sam) and exhibiting an ic50 of 9 μm and a ki of 26 μm. it binds to a novel pocket near the sam-binding site on nsp16, suggesting potential as a pan-coronavirus therapeutic [1].
Antifungal agent 73;化合物 Antifungal agent 73Antifungal agent 73 (2024/9/14)
簡(jiǎn)介:antifungal agent 73 (compound a32) effectively combats azole-resistant candidiasis by disrupting the fungal cell wall and membrane. it demonstrates potent in vivo activity against pathogenic fungi, including fluconazole-resistant strains [1].
SHP2-IN-16;化合物 SHP2-IN-16SHP2-IN-16 (2024/9/14)
簡(jiǎn)介:shp2-in-16 (compound 222) is a potent shp2 inhibitor exhibiting an ic50 of 1 nm, and is applicable in glioblastoma research [1].
hCAXII-IN-7;化合物 hCAXII-IN-7hCAXII-IN-7 (2024/9/14)
簡(jiǎn)介:hcaxii-in-7 (compound 6e) functions as an inhibitor of human carbonic anhydrase xii (hca xii) and possesses blood-brain barrier (bbb) permeability. moreover, it promotes apoptosis in 786-0, sf-539, and hs 578 t cell lines [1].
anti-TNBC agent-3;化合物 anti-TNBC agent-3anti-TNBC agent-3 (2024/9/14)
簡(jiǎn)介:anti-tnbc agent-3 (compound 3g) is a compound that induces apoptosis and possesses anti-cancer cell proliferation properties. it effectively inhibits tumor growth and metastasis in xenograft models of triple-negative breast cancer (tnbc) [1].
Imipramine hydrochloride;鹽酸丙咪嗪Imipramine (hydrochloride)|||Tofranil|||G 22355|||Imipramine HCl|||Mel (2024/9/14)
簡(jiǎn)介:imipramine hydrochloride (imipramine hcl) is a first generation tricyclic antidepressant that acts primarily as an inhibitor of serotonin and norepinephrine transporters (kds = 1.4 and 37 nm, respectively).imipramine hydrochloride is reported to prevent the translocation of asmase, inhibiting mv and exosomes secretion
Antibacterial agent 154;化合物 Antibacterial agent 154Antibacterial agent 154 (2024/9/14)
簡(jiǎn)介:antibacterial agent 154 (compound 7), a fluoroquinolone derivative, exhibits broad-spectrum efficacy against both gram-positive and gram-negative bacteria when administered orally. it has been shown to be effective in vivo using a mouse model of staphylococcal sepsis [1].
KGP591;化合物 KGP591KGP591 (2024/9/14)
簡(jiǎn)介:kgp591, a tubulin polymerization inhibitor with an ic50 of 0.57 μm, effectively induces g2/m arrest, inhibits cell migration, and disrupts microtubule structure and cell morphology in mda-mb-231 cells. additionally, it demonstrates antitumor activity in an orthotopic kidney cancer model (renca) [1].
HL23;化合物 HL23HL23 (2024/9/14)
簡(jiǎn)介:hl23 is a histone deacetylase (hdac) inhibitor that effectively targets hepatocellular carcinoma (hcc). it promotes acetylation at the txnip promoter and increases txnip expression, which in turn modulates potassium channel activity and induces txnip-dependent potassium deficiency. additionally, hl23 impedes the advancement and spread of hcc and demonstrates a synergistic effect when combined with sorafenib, exhibiting greater potency than the duo of sorafenib and vorinostat [1].
Tyrosinase-IN-14;化合物 Tyrosinase-IN-14Tyrosinase-IN-14 (2024/9/14)
簡(jiǎn)介:tyrosinase-in-14 (compound 7m), a tyrosinase inhibitor, modulates the enzyme´s secondary structure to diminish its catalytic function, exhibits low cytotoxicity, and possesses anti-browning properties that effectively prevent banana discoloration during storage [1].
PARP1-IN-15;化合物 PARP1-IN-15PARP1-IN-15 (2024/9/14)
簡(jiǎn)介:parp1-in-15 (compound 6) is a parp1 inhibitor that also inhibits tankyrase (tnks) and promotes dna double-strand breaks, leading to tumor cell apoptosis. it exhibits anti-cancer activity in triple-negative breast cancer (tnbc) cells and patient-derived organoids, making it useful for tnbc research, including cases with or without brca1 mutations [1].
A09-003;化合物 A09-003A09-003 (2024/9/14)
簡(jiǎn)介:a09-003 is a novel cell cycle protein-dependent kinase-9 cdk-9 inhibitor.a09-003 inhibits the proliferation of a variety of leukemia cell lines and inhibits the increase of leukemia sequence-1 protein in myeloid cells.a09-003 also induces apoptosis, decreases rna polymerase ii activity, and decreases mcl-1 expression.
VEGFR-2-IN-36;化合物 VEGFR-2-IN-36VEGFR-2-IN-36 (2024/9/14)
簡(jiǎn)介:vegfr-2-in-36 (compound 15) serves as a potent vegfr-2 inhibitor, exhibiting an ic50 value of 0.067 μm, and acts as an apoptosis inducer with demonstrated anticancer efficacy. it modulates apoptotic pathways by upregulating bax and downregulating bcl-2, leading to cytotoxic effects on cancer cell lines, including mcf-7 (ic50 = 0.42 μm) and hepg2 (ic50 = 0.22 μm) [1].
α-Amylase/α-Glucosidase-IN-4;化合物 α-Amylase/α-Glucosidase-IN-4α-Amylase/α-Glucosidase-IN-4 (2024/9/14)
簡(jiǎn)介:α-amylase/α-glucosidase-in-4 (compound 5), a dual inhibitor targeting α-amylase (amylases) and α-glucosidase (glucosidase), exhibits potent inhibition with ic50 values of 1.10 μm and 0.15 μm respectively. this compound is noted for its potential antidiabetic activity [1].
Tyrosinase-IN-13;化合物 Tyrosinase-IN-13Tyrosinase-IN-13 (2024/9/14)
簡(jiǎn)介:tyrosinase-in-13 (compound 3c), stemming from flurbiprofen, acts as a potent non-competitive inhibitor of tyrosinase, exhibiting ic50 and ki values of 68 μm and 36.3 μm respectively. this compound demonstrates cytotoxicity against several cancer cell lines, including hepatocellular carcinoma (hepg2), colorectal cancer (ht-29), and melanoma (b16f10) [1].
VEGFR-2-IN-35;化合物 VEGFR-2-IN-35VEGFR-2-IN-35 (2024/9/14)
簡(jiǎn)介:vegfr-2-in-35 (compound 7) is a potent inhibitor of vegfr-2, exhibiting an ic50 of 37 nm. additionally, it demonstrates inhibitory activity against mcf-7 and hct 116 cancer cell lines with ic50 values of 10.56 μm and 7.07 μm, respectively [1].
Milnacipran ((1S-cis) hydrochloride);左旋米那普林Levomilnacipran Hydrochloride;左旋米那普林|||Levomilnacipran Hy (2024/9/14)
簡(jiǎn)介:milnacipran (1s-cis) hydrochloride (levomilnacipran hydrochloride) is a serotonin-norepinephrine reuptake inhibitor (snri), treatment of fibromyalgia.
E2730;化合物 E2730E2730 (2024/9/14)
簡(jiǎn)介:e2730 is a selective and noncompetitive inhibitor of the gamma-aminobutyric acid (gaba) transporter 1 (gat1) that exhibits oral availability as well as antiepileptic properties. its inhibition of gat1 is dependent on the prevailing gaba concentrations and specifically targets gat1-mediated gaba uptake. demonstrating in vivo effectiveness, e2730 has been tested at doses ranging from 5-50 mg/kg orally in various models, including the rat amygdala kindling and the mouse corneal kindling models, as
Ancistrotecine B;化合物 Ancistrotecine BAncistrotecine B (2024/9/14)
簡(jiǎn)介:ancistrotecine b (compound 2), a nav1.7 channel inhibitor (ic50: 0.73 μm), has been shown to alleviate inflammatory pain in mice [1].
Neutrophil elastase inhibitor 4;化合物 Neutrophil elastase inhibitor 4Neutrophil elastase inhibitor 4 (2024/9/14)
簡(jiǎn)介:neutrophil elastase inhibitor 4 (compound 4f) is a competitive inhibitor of human neutrophil elastase (hne) with ic50 of 42.30 nm and ki of 8.04 nm. it prompts apoptosis in t47d cells and inhibits the proliferation of t47d, rpmi 8226, a549, and hsf cells with respective ic50 values of 21.25, 34.17, 29.93, and 99.11 nm [1].
T3SS-IN-2;化合物 T3SS-IN-2T3SS-IN-2 (2024/9/14)
簡(jiǎn)介:t3ss-in-2 (compound 2h) serves as an inhibitor of the type three secretion system (t3ss), with applications in bacterial infection research [1].
CBP/p300-IN-21;化合物 CBP/p300-IN-21CBP/p300-IN-21 (2024/9/14)
簡(jiǎn)介:cbp/p300-in-21 (compound 5d), a selective inhibitor of cbp/p300 with ic50 values of 0.07 μm for p300 and 1.755 μm for cbp, reduces h3k18ac levels and inhibits the growth of 4t1 tumors in mice [1].
ALK/EGFR-IN-3;化合物 ALK/EGFR-IN-3ALK/EGFR-IN-3 (2024/9/14)
簡(jiǎn)介:alk/egfr-in-3 is a dual alk and egfr inhibitor that demonstrates potent anti-proliferative effects on various cancer cell lines, including h1975, pc9, and baf3-eml4-alk, with respective ic50 values of 0.1360, 0.0332, and 0.0339 μm [1].
ALK/EGFR-IN-2;化合物 ALK/EGFR-IN-2ALK/EGFR-IN-2 (2024/9/14)
簡(jiǎn)介:alk/egfr-in-2 is a potent dual inhibitor targeting alk and egfr, promoting apoptosis and g0/g1 cell cycle arrest in cancer cells. it effectively suppresses proliferation in h1975, pc9, and baf3-eml4-alk cancer cell lines, demonstrating ic50s of 0.0034, 0.0065, and 0.0018 μm, respectively [1].
ALK/EGFR-IN-1;化合物 ALK/EGFR-IN-1ALK/EGFR-IN-1 (2024/9/14)
簡(jiǎn)介:alk/egfr-in-1 (compound 8l) is a dual inhibitor targeting both alk and egfr, effectively blocking their phosphorylation. it demonstrates potent inhibition of alk/egfr mutants with ic50 values of 4.3 nm for egfr l858r t790m in h1975 cells and 3.6 nm for eml4-alk in baf3 cells. this compound may be applicable in the research of non-small cell lung cancer (nsclc) [1].
FLT3-IN-21;化合物 FLT3-IN-21FLT3-IN-21 (2024/9/14)
簡(jiǎn)介:flt3-in-21 (compound lc-3), a potent flt3 inhibitor with an ic50 value of 8.4 nm, induces apoptosis and arrests the cell cycle in the g1 phase. it effectively inhibits the proliferation of flt3-itd-positive aml cells mv-4-11, with an ic50 of 5.3 nm. in murine models, a daily dose of 10 mg/kg flt3-in-21 markedly inhibited tumor growth in the mv-4-11 xenograft model, achieving a tumor growth inhibition (tgi) of 92.16% [1].
Antileishmanial agent-23;化合物 Antileishmanial agent-23Antileishmanial agent-23 (2024/9/14)
簡(jiǎn)介:antileishmanial agent-23 (compound g1/9), a potent and selective trypanothione reductase (tr) inhibitor, exhibits an ic50 of 2.24 ± 0.52 μm. it effectively inhibits the growth of leishmania, trypanosoma cruzi, and trypanosoma brucei [1].
Fingolimod;芬戈莫德FTY-720A|||FTY-720;2-氨基-2-[2-(4-辛基苯基)乙基]-1,3-丙二醇|||FTY-720A|||FTY-720|||芬戈莫德 (2024/9/14)
簡(jiǎn)介:fingolimod (fty-720a) is an antagonist of sphingosine 1-phosphate (s1p) (ic50 of 0.033 nm in k562 and nk cells).