9月
Akt/NF-κB/MAPK-IN-1；化合物 Akt/NF-κB/MAPK-IN-1Akt/NF-κB/MAPK-IN-1 (2024/9/14)
簡介：akt/nf-κb/mapk-in-1 (compound 2m) serves as a potent, orally active inhibitor targeting no with an ic50 of 7.70 μm and demonstrates low toxicity. this compound exerts anti-inflammatory effects by impeding the akt/nf-κb and mapk signaling pathways [1].
CP-07；化合物 CP-07CP-07 (2024/9/14)
簡介：cp-07 is a selective and effective protac cdk9 degrader (dc50: 43 nm), demonstrating inhibition of 22rv1 cell proliferation (ic50: 62 nm) and colony formation by attenuating levels of mcl-1 and c-myc. additionally, cp-07 has been shown to impede the growth of 22rv1 xenograft tumors and is applicable in prostate cancer research [1].
IHMT-PI3K-455；化合物 IHMT-PI3K-455IHMT-PI3K-455 (2024/9/14)
簡介：ihmt-pi3k-455 (compound 15u) is a potent, selective pi3kγ/δ dual inhibitor, demonstrating oral activity, with ic50 values of 7.1 nm for pi3kγ and 0.57 nm for pi3kδ. this compound inhibits akt phosphorylation and promotes tumor regression through the recruitment and activation of cd8+ t cells. it is utilized in cancer research [1].
Phosphatase-IN-1；Phosphatase 抑制劑 1Phosphatase-IN-1 (2024/9/14)
簡介：phosphatase-in-1 (compound ii-8), a propranolol derivative, acts as an inhibitor of phosphatidate phosphatase (pah). it binds to mopah1 with an affinity constant of 19.8 μm, demonstrating growth inhibition of plant pathogens and anti-fungal properties. notably, phosphatase-in-1 exhibits no toxicity towards rice seedlings and wheat heads [1].
HIV-IN-7；化合物 HIV-IN-7HIV-IN-7 (2024/9/14)
簡介：axl-in-16 (compound 4), an axl inhibitor, not only suppresses axl expression and hif activity but also triggers fruiting body formation in flammulina velutipes. this compound can be extracted from the "fruiting liquid (fl)" of hypholoma lateritium and hericium erinaceus [1].
AJH-836；化合物 AJH-836AJH-836 (2024/9/14)
簡介：ajh-836 is a compound that activates munc13-1 and pkc ε/α, demonstrating a dissociation constant (kd) of 4.5 nm for pkcα, and facilitates the translocation of munc13-1 from the cytoplasm to the plasma membrane. it is utilized in neurodegenerative disease research [1].
FGFR1 inhibitor-9；化合物 FGFR1 inhibitor-9FGFR1 inhibitor-9 (2024/9/14)
簡介：fgfr1 inhibitor-9 (compound 7) is an fgfr1 inhibitor with potent binding affinity, exhibiting an ic50 of 0.85 nm. it targets the atp-binding pocket of fgfr1 and demonstrates anticancer activity [1].
FGFR1 inhibitor-8；化合物 FGFR1 inhibitor-8FGFR1 inhibitor-8 (2024/9/14)
簡介：fgfr1 inhibitor-8 (compound 9), an fgfr1 inhibitor with an ic50 of 0.5 nm, binds to the atp-binding pocket of fgfr1 and exhibits anticancer activity [1].
FGFR1 inhibitor 7；化合物 FGFR1 inhibitor 7FGFR1 inhibitor 7 (2024/9/14)
簡介：fgfr1 inhibitor 7 (compound 5), a potent fgfr1 tyrosine kinase inhibitor, exhibits an ic50 of 0.33 nm against its target and demonstrates broad-spectrum cytotoxicity against human cancer cell lines. additionally, it inhibits molt3 cells with an ic50 of 2.1 μm [1].
Proanthocyanidins原花青素Procyanidin (2024/9/14)
簡介：proanthocyanidins is a natural product, used as antioxidant and anti-cancers agent.
JNK2-IN-1；化合物 JNK2-IN-1JNK2-IN-1 (2024/9/14)
簡介：jnk2-in-1 (compound j27), a selective jnk2 inhibitor with a dissociation constant (kd) of 79.2 μm, exhibits anti-inflammatory effects by attenuating tnf-α and il-6 secretion via inhibition of the nf-κb/mapk pathway. it effectively mitigates symptoms associated with lps-induced acute lung injury (ali) and sepsis [1].
AChE/BChE-IN-15；化合物 AChE/BChE-IN-15AChE/BChE-IN-15 (2024/9/14)
簡介：ache/bche-in-15 (compound 6d) serves as an inhibitor for both acetylcholinesterase (ache) and butyrylcholinesterase (bche), presenting inhibition constants (ic50) of 20 nm for ache and 220 nm for bche. it interacts with the catalytic anionic site (cas) and the peripheral anionic site (pas) within the enzymes´ active sites. ache/bche-in-15 is applicable in alzheimer’s disease research [1].
CVN417；化合物 CVN417CVN417 (2024/9/14)
簡介：cvn417 is an orally active antagonist of nachr containing the α6 subunit, modulating phasic dopaminergic neurotransmission in an impulse-dependent fashion. it inhibits ca(2+) efflux through nachr subunits, displaying ic50 values of 0.086 μm (α6), 2.56 μm (α3), and 0.657 μm (α4). cvn417 has shown efficacy in reducing resting tremor in rodent models, suggesting a potential to ameliorate movement disorders in conditions like parkinson´s disease [1].
LN5P45；化合物 LN5P45LN5P45 (2024/9/14)
簡介：ln5p45, an otub2 inhibitor (ic50: 2.3 μm), promotes monoubiquitination of otub2 at lysine 31 and is utilized in the study of tumor progression and metastasis [1].
D4R agonist-1；D4R激動劑1D4R agonist-1 (2024/9/14)
簡介：d4r agonist-1 is a selective and potent d4r partial agonist (ki:2.2 nm).d4r agonist-1 can be used to study neurological diseases.
ERD-3111；化合物 ERD-3111ERD-3111 (2024/9/14)
簡介：erd-3111 (compound 44), an orally active protac erα degrader (dc50: 0.5 nm), exhibits efficacy in inhibiting tumor growth in both the parental mcf-7 xenograft model harboring wild-type er and two esr1-mutated mouse models. this compound has utility in the investigation of er+ breast cancer [1].
Quorum Sensing-IN-3；Quorum Sensing抑制劑1QS-IN-1；QS-IN-1 (2024/9/14)
簡介：quorum sensing-in-3 (qs-in-1) is a compound with inhibitory effects on bacterial community sensing, which inhibits the exchange of information between bacteria and inhibits biofilm formation.
JT002；化合物 JT002JT002 (2024/9/14)
簡介：jt002 is an orally active nlrp3 inflammasome inhibitor that decreases the production of nlrp3-dependent proinflammatory cytokines (such as il-1β, il-1α, il-18) and pyroptosis, as well as inhibits the formation of the nlrp3 inflammasome complex. additionally, jt002 mitigates airway hyperresponsiveness and airway neutrophilia in mice [1].
IHC3；化合物 IHC3IHC3 (2024/9/14)
簡介：ihc3 is a competitive and reversible monoamine oxidase b (mao-b) inhibitor with an ic50 of 1.672 μm, which targets cys172 within the enzyme´s active site. it is utilized in the study of neurological diseases [1].
5-LOX-IN-5；化合物 5-LOX-IN-55-LOX-IN-5 (2024/9/14)
簡介：compound 29, also known as 5-lox-in-5, is a 5-lipoxygenase (5-lox) inhibitor with an inhibitory concentration 50 (ic50) of 56 nm, utilized in research pertaining to neurodegenerative diseases [1].
Indomethacin farnesil；吲哚美辛法呢酯Infree；吲哚美辛法呢酯|||Infree (2024/9/14)
簡介：indomethacin farnesil (infree) is a prodrug of indomethacin. it acts as a nonsteroidal anti-inflammatory drug (nsaid) and disease-modifying anti-rheumatic drug (dmard).
VEGFR-2-IN-33；化合物 VEGFR-2-IN-33VEGFR-2-IN-33 (2024/9/14)
簡介：vegfr-2-in-33 (compound 4d), a potent vegfr inhibitor with an ic50 value of 61.04 nm, demonstrates significant inhibition of hepg2 cell proliferation, achieving an ic50 of 4.31 nm. this compound is utilized for hepatocellular carcinoma (hcc) research [1].
HDAC-IN-63；化合物 HDAC-IN-63HDAC-IN-63 (2024/9/14)
簡介：hdac-in-63 (compound 63) is a dual flt3/hdac inhibitor with ic50 values of 0.844 nm for flt3 and 30.0 nm for hdac1. it effectively suppresses mv4-11 cell proliferation with an ic50 of 92 nm, induces apoptosis, and arrests the cell cycle in mv4-11 cells. this compound is applied in acute myeloid leukemia (aml) research [1].
AChE-IN-39；化合物 AChE-IN-39AChE-IN-39 (2024/9/14)
簡介：ache-in-39 (compound 7c), with an ic50 value of 0.058 μm, is an acetylcholinesterase (ache) inhibitor known for its dpph scavenging activity and potential to ameliorate cognitive impairments in an aluminum chloride (alcl3)-induced amnesia animal model, suggesting its usefulness in alzheimer´s disease research [1].
Anti-osteoporosis agent-4；化合物 Anti-osteoporosis agent-4Anti-osteoporosis agent-4 (2024/9/14)
簡介：anti-osteoporosis agent-4 (compound 11h) suppresses the differentiation of primary osteoclasts and attenuates rankl-induced osteoclastogenesis. it effectively inhibits osteoclast formation, demonstrating an ic50 value of 358.29 nm, and impedes the activation of the pi3k/akt and iκbα/nf-κb signaling pathways [1].
MOZ-IN-3；化合物 MOZ-IN-3MOZ-IN-3 (2024/9/14)
簡介：moz-in-3 (compound 6j), a potent kat6a (moz) acetyltransferase inhibitor with an ic50 of 30 nm, exhibits antitumor activity against multiple myeloid leukemia cell lines, including hl-60, u937, skno-1, and k562. this compound also demonstrates favorable metabolic stability and pharmacokinetics [1].
COH1；化合物 COH1COH1 (2024/9/14)
簡介：coh1 is a ribonucleotide reductase (rr) inhibitor utilized in research pertaining to cancer, mitochondrial diseases, and neurodegenerative disorders [1].
CDK2/Bcl2-IN-1；化合物 CDK2/Bcl2-IN-1CDK2/Bcl2-IN-1 (2024/9/14)
簡介：cdk2/bcl2-in-1 (compound 1) is a saponin-based inhibitor of cdk-2 (ic50=117.6 nm) that exhibits potent cytotoxic effects on cancer cells. additionally, it inhibits bcl-2 and promotes apoptosis in a549 lung cancer cells [1].
HBV-IN-36；化合物 HBV-IN-36HBV-IN-36 (2024/9/14)
簡介：hbv-in-36 (also known as compound 42) is a hepatitis b virus (hbv) inhibitor with an ic50 of 2 μm, exhibiting anti-hbv activity characterized by an ec50 of 0.58 μm [1].
PROTAC AR-NTD degrader 1；化合物 PROTAC AR-NTD degrader 1PROTAC AR-NTD degrader 1 (2024/9/14)
簡介：protac ar-ntd antagonist 1 (compound 18) is a small molecule belonging to the protein-targeting chimeras (protacs) that selectively targets the n-terminal domain (ar-ntd) of the androgen receptor variant ar-v7. by antagonizing ar-ntd, this compound effectively degrades ar-v7 protein and triggers apoptosis in prostate cancer (pc) cells, with degradation efficiencies in vcap cells recorded at 62.2% (1 μm) and 71.1% (5 μm), as noted in reference [1].
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