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PI3Kα-IN-6；化合物 PI3Kα-IN-6PI3Kα-IN-6 (2024/9/9)
簡介：pi3kα-in-6 (compound 5b) is a pi3kα inhibitor that exhibits anticancer effects without toxicity to normal cells. pi3kα-in-6 increases ros production, decreases mitochondrial membrane potential and induces apoptosis.
HDAC-IN-47；化合物 HDAC-IN-47HDAC-IN-47 (2024/9/9)
簡介：hdac-in-47 is an orally active histone deacetylase (hdac) inhibitor with ic50 values of 19.75 nm, 57.8 nm, 40.27 nm, 5.63 nm and 302.73 nm for hdac1, hdac2, hdac3, hdac6 and hdac8, respectively. hdac-in-47 can block the cell cycle in g2/m phase, inhibit autophagy, induce apoptosis using the bax/bcl-2 and caspase-3 pathways, and has anti-cancer activity in vivo.
VEGFR-2-IN-16；化合物 VEGFR-2-IN-16VEGFR-2-IN-16 (2024/9/9)
簡介：vegfr-2-in-16 (compound 15b) is a potent inhibitor of vegfr-2 (ic50: 86.36 nm) that exhibits antitumour effects.
HIV-1 inhibitor-31；化合物 HIV-1 inhibitor-31HIV-1 inhibitor-31 (2024/9/9)
簡介：hiv-1 inhibitor-31 (compound 4) is a potent inhibitor of hiv-1. hiv-1 inhibitor-31 can be used in the study of aids.
SC144；化合物SC144SC144 (2024/9/9)
簡介：sc144 is an orally active small-molecule gp130 inhibitor.
Chitinase-IN-4；化合物 Chitinase-IN-4Chitinase-IN-4 (2024/9/9)
簡介：chitinase-in-4 (compound 8f) is a potent and selective inhibitor of ofchi-h with an ic50 value of 0.1 μm and good insecticidal activity.
Chitin synthase inhibitor 1；化合物 Chitin synthase inhibitor 1Chitin synthase inhibitor 1 (2024/9/9)
簡介：chitin synthase inhibitor 1 is a potent and selective chitin synthase (chs) inhibitor with ic50 of 0.12 mm. chitin synthase inhibitor 1 potently inhibits drug-resistant fungi variants.
TRPC5-IN-3；化合物 TRPC5-IN-3TRPC5-IN-3 (2024/9/9)
簡介：trpc5-in-3 is a potent trpc5 inhibitor (ic50= 10.75 nm).
Antitubercular agent-29；化合物 Antitubercular agent-29Antitubercular agent-29 (2024/9/9)
簡介：antitubercular agent-29 (compound 6xa) is a potent drug resistant (dr) mycobacterium tuberculosis (mtb) inhibitor. antitubercular agent-29 exhibits mic of 0.03 μg/ml against drug-susceptible (ds)-mtb strains, mic of 0.03-0.06 μg/ml against dr-mtb strains. antitubercular has favourable selectivity (si>40) against vero cells.
c-ABL-IN-4；化合物 c-ABL-IN-4c-ABL-IN-4 (2024/9/9)
簡介：c-abl-in-4 is a potent inhibitor of c-abl.
PDE4B/7A-IN-2；化合物 PDE4B/7A-IN-2PDE4B/7A-IN-2 (2024/9/9)
簡介：this compound is a dual 5-ht1a/5-ht7 receptor antagonist (5-ht1a ki = 8 nm, kb = 0.04 nm; 5-ht7 ki = 451 nm, kb = 460 nm) with additional inhibitory activity against pde4b/pde7a (pde4b ic50 = 80.4 μm; pde7a ic50 = 151.3 μm). its antidepressant-like effect surpasses that of the reference agent, escitalopram.
Antibacterial agent 76；化合物 Antibacterial agent 76Antibacterial agent 76 (2024/9/9)
簡介：antibacterial agent 76 (compound 9) is a potent antibacterial agent.
MAO-B-IN-7；化合物 MAO-B-IN-7MAO-B-IN-7 (2024/9/9)
簡介：mao-b-in-7 is a potent and blood-brain barrier permeable mao-b and ache inhibitor. mao-b-in-7 exhibits ic50 s of 41 nm, 87 nm and 0.3 μm for human ache, electric eel ache and mao-b, respectively. mao-b-in-7 effectively alleviates oxidative stress and neuroinflammatory damage.
COX-2-IN-6；COX-2抑制劑6COX-2-IN-6 (2024/9/9)
簡介：cox-2-in-6 is a potent, selective, and orally available cyclooxygenase-2 (cox-2) inhibitor with an ic50 of 0.84 μm and a ki of 69 nm.cox-2-in-6 inhibits cox-2-driven pge2 synthesis with an ic50 of 0.60 μm.cox-2-in-6 is used to prevent colorectal cancer. cox-2-in-6 can be used to prevent colorectal cancer.
NF-κB-IN-5；化合物 NF-κB-IN-5NF-κB-IN-5 (2024/9/9)
簡介：nf-κb-in-5 (compound 4d) is an orally active nf-κb inhibitor. nf-κb-in-5 interacts directly with nf-κb. nf-κb-in-5 shows antitumor activity against human cancer cell lines, with ic 50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μm for hct116, u87-mg, hepg2, bgc823, pc9, respectively.
PHA-767491；化合物PHA767491CAY10572|||PHA767491|||PHA 767491；CAY10572|||PHA767491|||PHA 767491 (2024/9/9)
簡介：pha-767491 (cay10572) is a potent atp-competitive dual cdc7/cdk9 inhibitor with ic50 of 10 nm and 34 nm, respectively.
Influenza A virus-IN-6；化合物 Influenza A virus-IN-6Influenza A virus-IN-6 (2024/9/9)
簡介：influenza a virus-in-6 (compound 16j) is a potent and selective inhibitor of influenza a virus （ic 50= 3.88 μm, cc50= 36.64 μm). influenza a virus-in-6 exhibits anti-iav activity with low cytotoxicity.
αβ-Tubulin-IN-1；化合物 αβ-Tubulin-IN-1αβ-Tubulin-IN-1 (2024/9/9)
簡介：αβ-tubulin-in-1 is a potent and orally active inhibitor of αβ-tubulin. αβ- tubulin-in-1 blocks cell cycle at g2/m phase and induces apoptosis. αβ-tubulin-in-1 inhibits tumor cell migration and metastasis. αβ-tubulin-in-1 exhibits significant antitumor efficacy.
Anticancer agent 12；化合物 Anticancer agent 12Anticancer agent 12 (2024/9/9)
簡介：anticancer agent 12 shows cytotoxic activity in malignant cells with no hepatotoxicity.
(E/Z)-Zotiraciclib hydrochloride；化合物 (E/Z)-Zotiraciclib hydrochloride(E/Z)-Zotiraciclib hydrochlorid (2024/9/9)
簡介：(e/z)-zotiraciclib ((e/z)-tg02) hydrochloride is a potent inhibitor of cdk2, jak2, and flt3.
NVS-BET-1；化合物 NVS-BET-1NVS-BET-1 (2024/9/9)
簡介：nvs-bet-1 is a bet bromodomain inhibitor. nvs-bet-1 can regulate keratinocyte plasticity.
D4R antagonis-2；化合物 D4R antagonis-2D4R antagonis-2 (2024/9/9)
簡介：d4r antagonist-2 is a potent and selective d4r antagonist (ic50= 6.52 μm). d4r antagonist-2 displays favorable in vitro pk parameters and exhibits good brain penetration. d4r antagonist-2 has the research potential in parkinson’s disease.
Lorpucitinib；化合物L(fēng)orpucitinibJNJ-64251330；JNJ-64251330 (2024/9/9)
簡介：lorpucitinib (jnj-64251330) is an orally available, selective and potent jak kinase inhibitor for the study of inflammatory and gastrointestinal disorders associated with janus kinase (jak) signaling.
AMPK activator 6；化合物 AMPK activator 6AMPK activator 6 (2024/9/9)
簡介：ampk activator 6 (compound gc) activates the ampk pathway and reduces lipid content in hepg2 and 3t3-l1 cells. ampk activator 6 significantly suppresses the increase of total cholesterol (tc), low-density lipoprotein-c (ldl-c), triglyceride (tg), and other biochemical indices in blood serum. ampk activator 6 has research value in non-alcoholic fatty liver disease (nafld) and metabolic syndrome .
(R)-(+)-Dimethindene maleate；化合物 (R)-(+)-Dimethindene maleate(R)-(+)-Dimethindene maleate (2024/9/9)
簡介：(r)-(+)-dimethindene maleate is an orally active h 1 -receptor blocker.
Orexin receptor antagonist 4；化合物 Orexin receptor antagonist 4Orexin receptor antagonist 4 (2024/9/9)
簡介：orexin receptor antagonist 4 is potent and selective orexin 2 receptor (ox2r) antagonist. orexin receptor antagonist 4 shows ic50 of 4.27 nm and 295 nm for ox2r and ox1r, respectively.
AT7519；化合物AT7519AT7519 (2024/9/9)
簡介：at7519 is a cdk1/2/4/6/9 inhibitor (ic50: 10-210 nm). it is less effective to cdk3 and little active to cdk7.
CTX-712；化合物 CTX-712CTX-712 (2024/9/9)
簡介：ctx-712 is a potent inhibitor of cdc2-like kinase ( clk ). ctx-712 inhibits inhibits cancer survival and cancer cell growth.
Topo I-IN-1；化合物 Topo I-IN-1Topo I-IN-1 (2024/9/9)
簡介：topo i-in-1 (compound 14d) is a potent topo i inhibitor. topo i-in-1 exhibits antitumor activity and dna intercalative capability. topo i-in-1 can induce cell apoptosis.
pan-HER-IN-1；化合物 pan-HER-IN-1pan-HER-IN-1 (2024/9/9)
簡介：pan-her-in-1 (compound c5) is an irreversible, orally active pan- her inhibitor. pan-her-in-1 exhibits ic 50s of 0.38, 1.6, 2.2 and 3.5 nm for egfr, her4, egfr t790m/l858r and her2, respectively. pan-her-in-1 induces apoptosis and exhibits antitumor activities.
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