9月
SARS-CoV-2 Mpro-IN-7；化合物 SARS-CoV-2 Mpro-IN-7SARS-CoV-2 Mpro-IN-7 (2024/9/14)
簡介：sars-cov-2 mpro-in-7 (compound 6g) effectively inhibits sars-cov-2 main protease (mpro) with an ic50 value of 8.8 μm and exhibits a cytotoxic concentration (cc50) of 10 μm [1].
Cysteine protease inhibitor-3；化合物 Cysteine protease inhibitor-3Cysteine protease inhibitor-3 (2024/9/14)
簡介：cysteine protease inhibitor-3 (compound 15), a cysteine protease inhibitor, exhibits anti-plasmodial activity, effectively inhibiting pf3d7 (ic50 = 0.74 μm), pfw2 (ic50 = 1.05 μm), pffp2 (ic50 = 3.5 μm), and pffp3 (ic50 = 4.9 μm). it demonstrates efficacy against both drug-sensitive and drug-resistant parasites [1].
PAD4-IN-2；化合物 PAD4-IN-2PAD4-IN-2 (2024/9/14)
簡介：pad4-in-2 (compound 5i) is a pad4 inhibitor with an ic50 value of 1.94 μm, shown to suppress tumor growth in mice through specific inhibition of the pad4-h3cit-nets pathway in neutrophils [1].
Antiproliferative agent-25；化合物 Antiproliferative agent-25Antiproliferative agent-25 (2024/9/14)
簡介：antiproliferative agent-25 (compound 3s4) is a selective prmt5 inhibitor displaying an ic50 of 0.11 μm. it elevates hnrnp e1 protein levels and forms hydrogen bond interactions with sam and the e444 residue of prmt5. this compound exhibits antiproliferative effects in a549 cells by inducing apoptosis and inhibiting migration, albeit it presents high clearance rates, with half-lives of 21.8 minutes in human liver microsomes and 4.7 minutes in rat liver microsomes [1].
PRMT5-IN-31；化合物 PRMT5-IN-31PRMT5-IN-31 (2024/9/14)
簡介：prmt5-in-31 (compound 3m), a selective prmt5 inhibitor (ic50: 0.31 μm), increases hnrnp e1 protein levels by occupying the substrate site of prmt5 and establishing key interactions with amino acid residues. it exhibits antiproliferative properties against a549 cells through induction of apoptosis and inhibition of cell migration, while demonstrating high metabolic stability in human liver microsomes (t1/2: 132.4 min) [1].
NMDA receptor antagonist 6；化合物 NMDA receptor antagonist 6NMDA receptor antagonist 6 (2024/9/14)
簡介：nmda receptor antagonist 6 (compound 13b) functions as an antagonist at the glycine-binding site of the nmda receptor and demonstrates cytoneuroprotective efficacy. it safeguards pc12 cells from nmda-induced damage and apoptosis [1].
BDM91514；化合物 BDM91514BDM91514 (2024/9/14)
簡介：bdm91514 enhances antibiotic efficacy by inhibiting acrb, effectively curbing the proliferation of e. coli bw25113 with an ec90 of 8 μm when coupled with 8 μg/ml pyridomycin. additionally, bdm91514 exhibits favorable plasma and microsomal stability [1].
FGFR4-IN-14；化合物 FGFR4-IN-14FGFR4-IN-14 (2024/9/14)
簡介：fgfr4-in-14 (compound 27i) is a selective fgfr4 inhibitor with an ic50 of 2.4 nm, showing potent inhibition of cell proliferation in the v550l and n535k mutant strains. specifically, it registers ic50 values of 21 nm against huh7 cells, 2.5 nm against baf3/etv6-fgfr4-v550l cells, and 171 nm against baf3/etv6-fgfr4-n535k cells. demonstrating significant antitumor efficacy in the huh7 xenograft model, fgfr4-in-14 is utilized in the research of hepatocellular carcinoma (hcc) [1].
TMV-IN-6；化合物 TMV-IN-6TMV-IN-6 (2024/9/14)
簡介：tmv-in-6 (compound 4g) serves as a novel antiviral and fungicidal agent that impedes tobacco mosaic virus (tmv) assembly, functioning by attachment to tmv coat protein (cp) and disrupting the assembly interaction between tmv cp and rna [1].
β-Ionone；β-紫羅蘭酮β-lonone；乙位紫羅蘭酮|||β-紫羅蘭酮|||β-lonone (2024/9/14)
簡介：β-ionone (β-lonone) is an end-ring analog of β-carotenoids which widely distributed in fruit and vegetables,with anti-proliferative, anti-metastatic
TMV-IN-5；化合物 TMV-IN-5TMV-IN-5 (2024/9/14)
簡介：tmv-in-5 (compound 1a) serves as an antiviral/antifungal agent, specifically targeting and inhibiting the assembly of the tobacco mosaic virus (tmv) by binding to its coat protein (cp), hence its potential application in pesticide formulation [1].
Antihypertensive agent 3；化合物 Antihypertensive agent 3Antihypertensive agent 3 (2024/9/14)
簡介：antihypertensive agent 3 (compound 4a), an angiotensin ii receptor 1 antagonist, demonstrates antihypertensive activity in spontaneously hypertensive rats (shrs) [1].
Antihypertensive agent 2；化合物 Antihypertensive agent 2Antihypertensive agent 2 (2024/9/14)
簡介：antihypertensive agent 2 (compound 4g) exhibits effective antagonistic activities against angiotensin ii receptor 1 and reduces blood pressure with equal or greater potency than losartan [1].
Antitumor agent-104；化合物 Antitumor agent-104Antitumor agent-104 (2024/9/14)
簡介：antitumor agent-104 (compound 9) serves as an antineoplastic by impeding dna repair mechanisms in tumor cells, primarily through the inhibition of parp1 enzyme activity and reduction of par protein levels. additionally, it suppresses cdk12 expression [1].
Z1078601926；化合物 Z1078601926Z1078601926 (2024/9/14)
簡介：z1078601926 is an allosteric inhibitor of the human dopamine transporter (hdat) and exhibits a synergistic effect when combined with nomifensine [1].
Antitumor agent-102；化合物 Antitumor agent-102Antitumor agent-102 (2024/9/14)
簡介：antitumor agent-102 (compound 10), a conjugate integrating a topoisomerase i inhibitor sn38 with a glucose transporter inhibitor, specifically targets colorectal cancer. this agent facilitates elevated levels of free sn38 in tumor tissues compared to irinotecan [1].
SSI-4；化合物 SSI-4SSI-4 (2024/9/14)
簡介：ssi-4 is a stearoyl coa desaturase 1 (scd1) inhibitor that can be labeled with carbon-11 (11c) for use as a ligand in small animal in vivo pet/ct imaging studies of scd1 [1].
P-gp inhibitor 15；化合物 P-gp inhibitor 15P-gp inhibitor 15 (2024/9/14)
簡介：p-gp inhibitor 15 (compound 7a), a nonsubstrate inhibitor of p-glycoprotein (pgp), inhibits pgp-atpase activity and interferes with pgp-mediated rhodamine123 efflux. additionally, this compound enhances the inhibitory effect of paclitaxel on tumor progression in the kbv xenograft tumor model in nude mice [1].
MCI；化合物 MCIMCI (2024/9/14)
簡介：mci, a chemical compound demonstrating significant anti-inflammatory effects, particularly in collagen-induced arthritis (cia) models, modulates inflammation through macrophage reprogramming by enhancing ros scavenging and promoting cox-2 downregulation. it effectively inhibits cox-2, exhibiting an ic50 of 1.23 μm. additionally, mci holds potential for research applications in rheumatoid arthritis (ra) [1].
Carmoisine；偶氮玉紅Azo Rubine|||Chromotrope FB；Azo Rubine|||Chromotrope FB|||偶氮玉紅|||鉻變素FB (2024/9/14)
簡介：carmoisine (azo rubine) is a food dye azorubine and is used for the purposes where food is heat-treated after fermentation.
α-Glucosidase-IN-25；化合物 α-Glucosidase-IN-25α-Glucosidase-IN-25 (2024/9/14)
簡介：α-glucosidase-in-25 (compound (r)-8k) serves as a competitive inhibitor for α-glucosidase, demonstrating an inhibitory concentration 50 (ic50) of 1.19μm, making it applicable in anti-diabetic research [1].
sEH inhibitor-16；化合物 sEH inhibitor-16sEH inhibitor-16 (2024/9/14)
簡介：seh inhibitor-16, a potent soluble epoxide hydrolase (seh) inhibitor, exhibits an ic50 of 2 nm. it diminishes inflammatory damage associated with cerulein-induced acute pancreatitis (ap) in mice, making it suitable for inflammation and immunology research [1].
FGFR-IN-11；化合物 FGFR-IN-11FGFR-IN-11 (2024/9/14)
簡介：fgfr-in-11 (compound i-5) is an orally active, covalent inhibitor of fgfr, exhibiting ic50 values of 9.9 nm (fgfr1), 3.1 nm (fgfr2), 16 nm (fgfr3), and 1.8 nm (fgfr4). this compound demonstrates nanomolar potency in inhibiting proliferation of various cancer cells and significantly hinders tumor growth in xenograft mouse models [1].
DPP-4-IN-8；化合物 DPP-4-IN-8DPP-4-IN-8 (2024/9/14)
簡介：dpp-4-in-8 (compound 27) is a potent and selective inhibitor of dipeptidyl peptidase 4 (dpp4), with an inhibition constant (ki) of 0.96 μm. it inhibits the dipeptidase activity of dpp4 in both caco-2 and hepg-2 cells and dose-dependently reduces the expression of chemokines such as tumor necrosis factor-α (tnf-α), interleukin-6 (il-6), and interleukin-1β (il-1β) [1].
UPCDC30766；化合物 UPCDC30766UPCDC30766 (2024/9/14)
簡介：upcdc30766, a potent allosteric inhibitor of p97, exhibits an ic50 of 12 nm and is applicable for colon cancer research [1].
Antitrypanosomal agent 14；化合物 Antitrypanosomal agent 14Antitrypanosomal agent 14 (2024/9/14)
簡介：antitrypanosomal agent 14 (compound 1), a potent t. brucei inhibitor with an effective concentration (ec50) of 0.47 μm, also inhibits tb gsk3 with an inhibitory concentration (ic50) of 12 μm, and is utilized in the research of human african trypanosomiasis [1].
HAT-IN-8；化合物 HAT-IN-8HAT-IN-8 (2024/9/14)
簡介：hat-in-8 (compound 38), a blood-brain barrier-permeable inhibitor of trypanosoma brucei with an ec50 of 0.18 μm, is utilized in the study of human african trypanosomiasis [1].
Apoptosis inducer 13；化合物 Apoptosis inducer 13Apoptosis inducer 13 (2024/9/14)
簡介：apoptosis inducer 13 (compound ru4) promotes apoptosis in cancer cells while also suppressing their migration and invasion. additionally, it facilitates the conversion of coenzyme nadh to nad+, and elevates intracellular ros levels [1].
AChE-IN-30；化合物 AChE-IN-30AChE-IN-30 (2024/9/14)
簡介：ache-in-30 is an acetylcholinesterase (ache) inhibitor exhibiting neuroprotective effects with an inhibitory concentration (ic 50) of 4.4 μm. it prevents hydrogen peroxide (h 2 o 2)-induced apoptosis by inhibiting the accumulation of reactive oxygen species (ros) within cells and is utilized in alzheimer´s disease research [1].
PROTAC α-synuclein degrader 5；化合物 PROTAC α-synuclein degrader 5PROTAC α-synuclein degrader 5 (2024/9/14)
簡介：protac α-synuclein degrader 5 is a highly selective (protac) compound that targets and degrades α-synuclein aggregates, exhibiting an dc50 value of 7.51 μm and achieving a maximum degradation rate (dmax) of 89%. the compound incorporates the probe molecule sery308 and e3 ligase ligands, making it suitable for neurological disease research [1].
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