9月
LZWL02003；化合物 LZWL02003LZWL02003 (2024/9/14)
簡介：lzwl02003, an anti-neuroinflammatory agent, demonstrates a protective effect on mpp+-induced neuronal damage and reduces ros expression. additionally, it enhances cognition, memory, learning, and athleticism in rotenone-induced parkinson´s disease (pd) rat models, suggesting its potential for neurodegenerative disease research [1].
Antiproliferative agent-32；化合物 Antiproliferative agent-32Antiproliferative agent-32 (2024/9/14)
簡介：antiproliferative agent-32 (compound 1c) impedes phosphorylation within the pi3k/akt/mtor signaling pathway, restrains proliferation of huh7 and sk-hep-1 cells, induces apoptosis, and inflicts mitochondrial damage, rendering it a potential subject for hepatocellular carcinoma research [1].
Antioxidant agent-13；化合物 Antioxidant agent-13Antioxidant agent-13 (2024/9/14)
簡介：compound 5f (antioxidant agent-13) is an antioxidant that demonstrates inhibition of dpph and frap with half maximal inhibitory concentrations (ic50s) of 80.33 μm and 85.69 μm, respectively. additionally, it inhibits the enzymes lipoxygenase (lox) and xanthine oxidase (xo) with ic50s of 16.85 μm and 23.01 μm, respectively [1].
PARP-1-IN-13；化合物 PARP-1-IN-13PARP-1-IN-13 (2024/9/14)
簡介：parp-1-in-13 (compound 19c) is a potent parp-1 inhibitor with an ic50 of 26 nm, hindering dna single-strand break repair and exacerbating dna double-strand breaks. it induces apoptosis in cancer cells via the mitochondrial pathway [1].
D(+)-LACTIDE；D丙交酯D(+)-LACTIDE (2024/9/14)
簡介：d(+)-lactide is a cyclic dimer of acetone used in the synthesis of a variety of drugs and other compounds, as well as in biochemical and physiological studies.
SARS-CoV-2-IN-56；化合物 SARS-CoV-2-IN-56SARS-CoV-2-IN-56 (2024/9/14)
簡介：sars-cov-2-in-56 (compound 63) is a sars-cov-2 inhibitor with antiviral activity, demonstrating inhibition of the virus in vero e6 cells with an ic50 of 0.7 μm [1].
SARS-CoV-2-IN-54；化合物 SARS-CoV-2-IN-54SARS-CoV-2-IN-54 (2024/9/14)
簡介：sars-cov-2-in-54 (compound 2), a sars-cov-2 inhibitor, exhibits antiviral activity by impeding the virus in vero e6 cells with an inhibitory concentration (ic50) of 21.4 μm [1].
EGFR-IN-81；化合物 EGFR-IN-81EGFR-IN-81 (2024/9/14)
簡介：egfr-in-81 (compound 10i), an egfr inhibitor, demonstrates potent activity by inhibiting egfr wt and the l858r/t790m mutation at ic50 values of 4.38 nm and 5.69 nm, respectively. it also exhibits cytotoxic effects against mcf-7 and hct116 cell lines with ic50 values of 2.07 μm and 6.72 μm, respectively [1].
MRS7925；化合物 MRS7925MRS7925 (2024/9/14)
簡介：mrs7925 (compound 43) serves as a potent antagonist of the 5-ht2b receptor, with an inhibition constant (ki) of 17 nm, and is utilized in the study of fibrosis [1].
5-HT6 agonist 1；化合物 5-HT6 agonist 15-HT6 agonist 1 (2024/9/14)
簡介：compound 19, a 5-ht6 agonist with an affinity (k i : 5 nm), exhibits antidepressant-like effects and enhances cognitive function while also inhibiting platelet aggregation. it demonstrates high metabolic stability [1].
HIV-1 inhibitor-59；化合物 HIV-1 inhibitor-59HIV-1 inhibitor-59 (2024/9/14)
簡介：hiv-1 inhibitor-59 (compound i-5b) effectively inhibits both wild-type and mutant strains of hiv-1, with ec50 values ranging from 5.62 to 171 nm. additionally, it demonstrates moderate inhibitory activity against the reverse transcriptase (rt) enzyme, with ic50 values between 0.094 and 12.0 μm [1].
PROTAC Hsp90α degrader 1；化合物 PROTAC Hsp90α degrader 1PROTAC Hsp90α degrader 1 (2024/9/14)
簡介：compound x10g (protac hsp90α degrader 1) is a selective agent targeting hsp90α for degradation and is utilized in breast cancer research. it demonstrates inhibitory effects on the proliferation of breast cancer cell lines, mda-mb-231, mda-mb-468, mcf-7, and mx-1, with respective ic50 values of 51.48 μm, 16.46 μm, 8.93 μm, and 11.95 μm [1].
Antiproliferative agent-30；化合物 Antiproliferative agent-30Antiproliferative agent-30 (2024/9/14)
簡介：antiproliferative agent-30 (compound 8g) demonstrates broad-spectrum antiproliferative activity, with ic50 values of 0.054 nm, 0.008 nm, and 0.144 nm against hct-116, k562, and mv-4-11 cancer cell lines, respectively. it inhibits tubulin assembly as well as flt3 and abl1 kinases and exhibits vascular-disrupting capabilities. additionally, it exerts an anticancer effect against acute myeloid leukemia (aml) with flt3-itd-tkd mutations [1].
nSMase2-IN-1；化合物 nSMase2-IN-1nSMase2-IN-1 (2024/9/14)
簡介：nsmase2-in-1 is an orally active inhibitor of neutral sphingomyelinase 2 (nsmase2) with a potent ic50 value of 0.13 ± 0.06 μm. it demonstrates metabolic stability in liver microsomes and possesses a favorable brain-to-plasma ratio, indicating effective oral bioavailability. this compound is utilized in nervous system disease research [1].
Antitumor agent-114；化合物 Antitumor agent-114Antitumor agent-114 (2024/9/14)
簡介：antitumor agent-114, a potent sting (stimulator of interferon genes) agonist, activates immune responses and diminishes tumor size in mouse breast cancer models, demonstrating potential applications in immunity and cancer research [1].
[(2-Methoxyphenoxy)Methyl]Oxirane；愈創(chuàng)木酚縮水甘油醚[(2-Methoxyphenoxy)Methyl]Oxirane (2024/9/14)
簡介：[(2-methoxyphenoxy)methyl]oxirane is a natural product.
OATD-02；化合物 OATD-02OATD-02 (2024/9/14)
簡介：oatd-02 is an orally active, competitive, reversible, noncovalent inhibitor with slow offset kinetics that targets both arginase1 and 2, exhibiting inhibitory concentrations (ic50) of 20 nm (harg1), 39 nm (harg2), 39 nm (marg1), and 28 nm (rarg1). notably, oatd-02 mitigates tumor immunosuppression provoked by these arginases and has potential application in melanoma research [1].
α-Glucosidase-IN-30；化合物 α-Glucosidase-IN-30α-Glucosidase-IN-30 (2024/9/14)
簡介：α-glucosidase-in-30 (compound 8c) is a potent, orally active competitive inhibitor of α-glucosidase, exhibiting a k i of 40.0 μm and an ic50 of 49.0 μm. it is non-cytotoxic to both cancerous mcf-7 and normal hdf cell lines, rendering it suitable for type 2 diabetes research [1].
MBL-IN-1；化合物 MBL-IN-1MBL-IN-1 (2024/9/14)
簡介：mbl-in-1 (compound 41), a β-lactamase inhibitor, exhibits an ic50 range of 0.10 to 25.85 μm and is utilized in the study of bacterial infections [1].
Antitrypanosomal agent 15；化合物 Antitrypanosomal agent 15Antitrypanosomal agent 15 (2024/9/14)
簡介：antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor of the trypanosoma cruzi proteasome, exhibiting a pic50 of 7.4 for t. cruzi and <4 for the human proteasome. it possesses favorable adme properties, rendering it useful for the study of chagas disease [1].
PROTAC TG2 degrader-2；化合物 PROTAC TG2 degrader-2PROTAC TG2 degrader-2 (2024/9/14)
簡介：protac tg2 degrader-2 (compound 7) is a selective competitive degrader of transglutaminase 2 (tg2), exhibiting a dissociation constant (kd) greater than 100 μm. it inhibits cell migration and reduces tg2 levels in ovarian cancer cells, making it a valuable tool for ovarian cancer research [1].
PD-L1-IN-3；化合物 PD-L1-IN-3PD-L1-IN-3 (2024/9/14)
簡介：pd-l1-in-3 (compound 4a) functions as an inhibitor targeting the pd-1/pd-l1 axis, with an ic50 value of 4.97nm for pd-l1 inhibition and an ec50 value of 2.70 μm for jurkat t cell modulation. it antagonizes the pd-1/pd-l1 interaction by binding to the pd-l1 dimer, obstructing pd-1 signaling. this compound is utilized in research pertaining to lung cancer and melanoma [1].
BI 7446；化合物 BI 7446BI 7446 (2024/9/14)
簡介：bi 7446 is a potent and selective cyclic dinucleotide (cdn)-based stimulator of interferon genes (sting) agonist capable of activating all five sting variants in cells, thus inducing tumor-specific immune-mediated tumor rejection. this compound is utilized in immuno-oncology research [1].
FGH31；化合物 FGH31FGH31 (2024/9/14)
簡介：fgh31 (compound 24), a dopamine d4 agonist, exhibits potent and selective grk2-dependency with a k i of 1.6 nm and partially activates β-arrestin [1].
CNBCA；化合物 CNBCACNBCA (2024/9/14)
簡介：cnbca, a selective and potent competitive inhibitor of the shp2 enzyme, exhibits an ic50 value of 0.87 μm. it binds to the full-length shp2, effectively inhibiting its enzyme activity, as well as impeding pakt and perk1/2. furthermore, cnbca suppresses the proliferation of bt474 and mda-mb468 cells, indicating potential utility in breast cancer research [1].
SARS-CoV-2-IN-53；化合物 SARS-CoV-2-IN-53SARS-CoV-2-IN-53 (2024/9/14)
簡介：ars-cov-2-in-53 (compd 5d) exhibits an inhibitory effect on sars-cov-2 replication, with an effective concentration (ec50) value of 14.3 μm, and demonstrates notable antiviral activity against human coronavirus 229e (hcov-229e) [1].
16a,17a-Epoxy-4-Pregnen-3,20-Dione；16,17-環(huán)氧黃體酮16a,17a-Epoxy-4-Pregnen-3,20-Dione (2024/9/14)
簡介：16a,17a-epoxy-4-pregnen-3,20-dione is a synthetic progestin, a metabolite of the luteinizing hormone hormone, which acts by binding to the luteinizing hormone receptor. it has been used to study the effects of progesterone on reproductive organs, the effects of the hormone on cell growth and development, and the effects of the hormone on the immune system.
Antibacterial agent 149；化合物 Antibacterial agent 149Antibacterial agent 149 (2024/9/14)
簡介：compd 3j (antibacterial agent 149) is a laccase inhibitor that exhibits potent fungicidal activity, particularly useful in researching rice sheath blight [1].
DNA polymerase-IN-3；化合物 DNA polymerase-IN-3DNA polymerase-IN-3 (2024/9/14)
簡介：dna polymerase-in-3 (compd 5b), a coumarin derivative, demonstrates inhibitory activity against taq dna polymerase and has potential applications in proliferative disease research [1].
DNA polymerase-IN-2；化合物 DNA polymerase-IN-2DNA polymerase-IN-2 (2024/9/14)
簡介：dna polymerase-in-2 (compd 3c), a coumarin derivative, demonstrates inhibitory activity towards taq dna polymerase, with an ic50 value of 48.25 μm, and holds potential for application in value-added disease research [1].
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