9月
LTB4-IN-2；化合物 LTB4-IN-2LTB4-IN-2 (2024/9/14)
簡介：ltb4-in-2 (compound 6x) is a selective inhibitor of leukotriene b4 (ltb4), acting by specifically targeting the 5-lipoxygenase-activating protein (flap) with an inhibitory concentration (ic 50) of 1.15 μm, thus serving as a potential agent for anti-inflammatory research [1].
Anticancer agent 154；化合物 Anticancer agent 154Anticancer agent 154 (2024/9/14)
簡介：anticancer agent 154 (compound 8h) enhances reactive oxygen species production, causing mitochondrial damage, and promotes cell apoptosis and dna damage. it triggers ferroptosis by depleting gsh, diminishing gpx4 expression, and escalating lipid peroxidation. furthermore, it effectively suppresses the proliferation of various cancer cells (ht29, h1975, a549, and mcf-7) with ic50 values ranging from 1.0 to 1.9 μm [1].
YJ182；化合物 YJ182YJ182 (2024/9/14)
簡介：yj182 is an ndm-1 inhibitor with an ic50 of 0.23 μm, and additionally inhibits imp-1, vim-2, gim-1, and mmp-2 with respective ic50 values of 0.25, 0.61, 0.49, and 6.92 μm. it is utilized in bacterial infection research [1].
EGFR-IN-84；化合物 EGFR-IN-84EGFR-IN-84 (2024/9/14)
簡介：egfr-in-84 (compound 6g), an egfr inhibitor with an ic50 of 24 nm, impedes the growth of a549 cells with an ic50 value of 1.537 μm and is utilized for lung cancer research [1].
PDE1-IN-5；化合物 PDE1-IN-5PDE1-IN-5 (2024/9/14)
簡介：pde1-in-5 (compound 10c) is a selective pde1c inhibitor with an ic50 of 15 nm, exhibiting anti-inflammatory properties through the inhibition of inos, tnf-α, il-1α, il-1β, and il-6 expression induced by lps. it has demonstrated efficacy in mitigating inflammatory bowel disease (ibd) symptoms in a dextran sodium sulfate (dss)-induced colitis mouse model, suggesting its potential utility for ibd research [1].
Antifungal agent 72；化合物 Antifungal agent 72Antifungal agent 72 (2024/9/14)
簡介：antifungal agent 72 (compound b8) demonstrates potent activity by inhibiting the efflux pump function and downregulating resistance-associated genes via disruption of the pdr1-kix interaction (k i : 11.7 μm). it exhibits efficacy against fluconazole-resistant strains, evidenced by a mic of 63 ng/ml, and displays synergistic effects when combined with fluconazole. this compound is particularly useful for researching c. glabrata infections [1].
ER degrader 7；化合物 ER degrader 7ER degrader 7 (2024/9/14)
簡介：er degrader 7 (compound 35t) is a selective degrader of both erα and erβ, and possesses activity as a tubulin polymerization inhibitor. it exhibits potent cell viability inhibition, with ic50 values of 0.06 μm for mcf-7, 2.56 μm for t47d, 15.84 μm for mcf-10a, 1.59 μm for lcc2, 1.67 μm for t47d d538g, and 1.37 μm for t47d y537s cells. additionally, er degrader 7 demonstrates efficacy in suppressing breast cancer tumor growth [1].
ER degrader 6；化合物 ER degrader 6ER degrader 6 (2024/9/14)
簡介：er degrader 6 (compound 35s) is a potent selective estrogen receptor modulator (serm) with the capacity to degrade estrogen receptor (er)α. it disrupts the microtubule network, inhibiting tubulin polymerization, and effectively suppresses tumor growth with minimal toxicity [1].
Galectin-3/galectin-8-IN-2；化合物 Galectin-3/galectin-8-IN-2Galectin-3/galectin-8-IN-2 (2024/9/14)
簡介：galectin-3/galectin-8-in-2 (compound 57) is a dual inhibitor targeting the c-terminal domains of galectin-3 and galectin-8, exhibiting dissociation constants (kd) of 12.8 μm and 2.06 μm, respectively. it effectively inhibits the migration of mrc-5 lung fibroblast cells and serves as a potential research tool for studying cancer and tissue fibrosis [1].
Galectin-3/galectin-8-IN-1；化合物 Galectin-3/galectin-8-IN-1Galectin-3/galectin-8-IN-1 (2024/9/14)
簡介：galectin-3/galectin-8-in-1 (compound 53) serves as a dual inhibitor of the galectin-3 and galectin-8 c-terminal domains, exhibiting dissociation constants (kd) of 4.12 μm for galectin-3 and 6.04 μm for galectin-8. it effectively impedes the migration of mrc-5 lung fibroblast cells and is utilized in cancer and tissue fibrosis research [1].
Quinidine奎尼丁奎尼丁|||奎寧樹 (2024/9/14)
簡介：quinidine is a stereoisomer of the antimalarial agent quinine and a class ia antiarrhythmic agent. for the treatment of abnormal heart rhythms and also malaria.
Antitubercular agent-39；化合物 Antitubercular agent-39Antitubercular agent-39 (2024/9/14)
簡介：antitubercular agent-39 (compound p1) is a potent agent effective against both drug-resistant strains and drug-susceptible clinical isolates of tuberculosis, exhibiting inhibition of the mtb strain h37rv with a minimum inhibitory concentration (mic) of less than 1 μm [1].
IIIM-8；化合物 IIIM-8IIIM-8 (2024/9/14)
簡介：iiim-8 is a melanogenesis inhibitor that suppresses pigment production in both in vitro and in vivo settings, exhibiting no cytotoxic effects on human adult epidermal melanocytes (haem). it has potential applications in the study of hyperpigmentation disorders [1].
NWP-0476；化合物 NWP-0476NWP-0476 (2024/9/14)
簡介：nwp-0476 is a modified bcl-2/bcl-xl inhibitor with enhanced specificity for bcl-xl, suitable for research on relapsed t-acute lymphoblastic leukemia (t-all) [1].
SARS-CoV-2 3CLpro-IN-19；化合物 SARS-CoV-2 3CLpro-IN-19SARS-CoV-2 3CLpro-IN-19 (2024/9/14)
簡介：sars-cov-2 3clpro-in-19 (compound c5a), a non-covalent, non-peptide inhibitor of the sars-cov-2 3clpro enzyme, exhibits potent in vitro activity with an ic50 of 0.7 μm. it demonstrates broad-spectrum efficacy against infection by omicron subvariants (ba.5, bq.1.1, and xbb.1.5) in human cells, with ec50 values ranging from 30-69 nm [1].
NMDA receptor antagonist 8；化合物 NMDA receptor antagonist 8NMDA receptor antagonist 8 (2024/9/14)
簡介：compound (r)-10a, an nmda receptor antagonist, exhibits selectivity for the glun2b subunit, possessing a ki of 265 nm and an ic50 of 62 nm. this compound is utilized in research pertaining to neurodegenerative diseases [1].
NMDA receptor antagonist 7；化合物 NMDA receptor antagonist 7NMDA receptor antagonist 7 (2024/9/14)
簡介：compound (s)-10a, a glun2b subunit-selective nmda receptor antagonist, exhibits a k i of 93 nm and an ic 50 of 72 nm. it is potentially useful for research into neurodegenerative diseases [1].
A3AR agonist 2；化合物 A3AR agonist 2A3AR agonist 2 (2024/9/14)
簡介：compound 19, a selective a3 adenosine receptor (a3ar) agonist (k i : 22.1 nm), effectively stimulates β-arrestin2 recruitment with an ec 50 value of 4.36 nm. this compound is utilized in research pertaining to inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, and other chronic conditions [1].
A3AR agonist 1；化合物 A3AR agonist 1A3AR agonist 1 (2024/9/14)
簡介：a3ar agonist 1 (compound 12), with a ki of 25.8 nm, is a potent a3 adenosine receptor (a3ar) agonist that promotes β-arrestin2 recruitment with an effective concentration (ec50) of 5.17 nm. it serves as a research tool in various pathological conditions, including inflammatory diseases, ischemia, cancer, neuropathic pain, and liver diseases [1].
HDAC-IN-62；化合物 HDAC-IN-62HDAC-IN-62 (2024/9/14)
簡介：hdac-in-62 (compound 5), an hdac inhibitor, exhibits ic50 values of 0.78, 1.0, and 1.2 μm for hdac6, hdac8, and hdac11, respectively. this compound suppresses microglial activation via autophagy induction and reduces nitric oxide production, demonstrating anti-inflammatory and antidepressant properties. additionally, hdac-in-62 has been shown to inhibit microglial activation in mouse brains [1].
FD2056；化合物 FD2056FD2056 (2024/9/14)
簡介：fd2056 is a potent, orally active pi3k inhibitor, with ic50 values of 0.30, 0.80, 1.10, and 0.42 nm against pi3kα, pi3kβ, pi3kγ, and pi3kδ, respectively. additionally, it exhibits inhibitory effects on cdk2-cyclina2 and cdk4-cyclind3 with ic50s of 115.95 nm and 2782.15 nm. fd2056 effectively inhibits the proliferation of various breast cancer cell lines, such as mda-mb-231, mda-mb-468, and mcf-7, with ic50s of 1.06 μm, 0.04 μm, and 1.40 μm, respectively. the compound also promotes apoptosis in c
ZMF-23；化合物 ZMF-23ZMF-23 (2024/9/14)
簡介：zmf-23, a pak1/hdac6 dual inhibitor, suppresses pak1 and hdac6-mediated aerobic glycolysis and cellular migration while inducing tnf-α-regulated necroptosis and augmenting apoptosis. the compound effectively hampers the warburg effect and cell motility, positioning it as a potential research tool for triple-negative breast cancer (tnbc) [1].
Antiproliferative agent-34；化合物 Antiproliferative agent-34Antiproliferative agent-34 (2024/9/14)
簡介：antiproliferative agent-34 (compound a14), a multitarget kinase inhibitor, demonstrates ic50 values of 177 nm for egfr l858r/t790m and 1567 nm for egfr wt. additionally, it inhibits jak2, ros1, flt3, flt4, and pdgfrα with respective ic50s of 30.93 nm, 106.90 nm, 108.00 nm, 226.60 nm, and 42.53 nm. in normoxic conditions, it suppresses the proliferation of h1975 and hcc827 cells with ic50 values below 40 nm, while under hypoxic conditions, its potency increases 4-6 fold, yielding ic50 values less
CDK9-IN-27；化合物 CDK9-IN-27CDK9-IN-27 (2024/9/14)
簡介：cdk9-in-27 (compound 6a), a cdk9 inhibitor with an ic50 of 0.424 μm, induces apoptosis and s-phase cell cycle arrest. it exhibits cytotoxicity against hepg2, hct-116, and mcf-7 cell lines, with ic50 values ranging from 10.31 to 40.34 μm, rendering it applicable in cancer research [1].
SP-2-225；化合物 SP-2-225SP-2-225 (2024/9/14)
簡介：sp-2-225, a selective inhibitor of hdac6, augments the production of cancer-associated antigens and enhances macrophage antigen cross-presentation to t cells, demonstrating a reduction in tumor volume within a syngeneic sm1 melanoma model [1].
TIM-3-IN-2；TIM-3 抑制劑2TIM-3-IN-2 (2024/9/14)
簡介：tim-3-in-2 is a tim3 inhibitor that inhibits the binding of tim-3 to ptdser, ceacam1, and gal-9 and inhibits the action of tim-3.tim-3-in-2 is able to reverse tim-3-mediated pro-inflammatory cytokine action.
Antiangiogenic agent 4；化合物 Antiangiogenic agent 4Antiangiogenic agent 4 (2024/9/14)
簡介：compound 3b, an antiangiogenic agent, inhibits akt phosphorylation in both hff and huvec cells and is utilized in cancer research [1].
APG-2449；化合物 APG-2449APG-2449 (2024/9/14)
簡介：apg-2449 is an orally active inhibitor targeting alk, ros1, and fak, demonstrating antitumor efficacy in mouse models of non-small cell lung cancer (nsclc) [1].
COX-2/15-LOX-IN-4；化合物 COX-2/15-LOX-IN-4COX-2/15-LOX-IN-4 (2024/9/14)
簡介：cox-2/15-lox-in-4 (compound 5i) is a dual inhibitor with ic50 values of 0.075 μm for cox-2 and 1.97 μm for 15-lox. it inhibits lps-induced production of pro-inflammatory cytokines (il-6, ros) and exhibits targeted anti-inflammatory effects [1].
COX-2/15-LOX-IN-3；化合物 COX-2/15-LOX-IN-3COX-2/15-LOX-IN-3 (2024/9/14)
簡介：cox-2/15-lox-in-3 (compound 5k) serves as a dual inhibitor for cox-2 and 15-lox, demonstrating inhibitory concentrations (ic50) of 0.075 μm and 1.97 μm, respectively. this compound effectively suppresses lps-induced cellular production of pro-inflammatory cytokines (il-6, ros, and no), exhibiting targeted anti-inflammatory effects [1].
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