9月
AM841；化合物 AM841AM841 (2024/9/14)
簡(jiǎn)介：am841, a high-affinity electrophilic ligand, covalently interacts with a cysteine residue in helix six, thus activating the cb1 cannabinoid receptor. it diminishes forskolin-stimulated camp accumulation and slows gastrointestinal motility [1] [2].
NNRTIs-IN-1；化合物 NNRTIs-IN-1NNRTIs-IN-1 (2024/9/14)
簡(jiǎn)介：nnrtis-in-1 is a potent non-nucleoside reverse transcriptase inhibitor (nnrti) with notable anti-resistance efficacy, effectively inhibiting both the wild-type hiv-1 and five mutant strains at ec50 values within the nanomolar range. this compound also exhibits favorable pharmacokinetic properties [1].
CST626；化合物 CST626CST626 (2024/9/14)
簡(jiǎn)介：cst626 (compound 9), a pan-iap degrader protac, effectively degrades xiap, ciap1, and ciap2 in mm.1s cells with dc50 values of 0.7, 2.4, and 6.2 nm, respectively [1].
MAT2A-IN-10；化合物 MAT2A-IN-10MAT2A-IN-10 (2024/9/14)
簡(jiǎn)介：mat2a-in-10 (compound 28), an orally active inhibitor of mat2a, exhibits an ic50 of 26 nm and is utilized in cancer research [1].
WCA-814；化合物 WCA-814WCA-814 (2024/9/14)
簡(jiǎn)介：wca-814, an androgen receptor (ar) antagonist-hsp90 inhibitor conjugate, induces degradation of both full-length and ar-v7, exhibiting cytotoxic effects in prostatic cancer cells with half maximal inhibitory concentrations (ic50) of 171.2 nm and 26.5 nm for lncap and 22rv1 cells, respectively [1].
VDR agonist 2；化合物 VDR agonist 2VDR agonist 2 (2024/9/14)
簡(jiǎn)介：vdr agonist 2 (compound 16i), a vitamin d receptor (vdr) agonist, effectively inhibits tgf-β1-induced hepatic stellate cell (hsc) activation, demonstrating notable anti-hepatic fibrosis efficacy both in vitro and in vivo [1].
Syk-IN-7；化合物 Syk-IN-7Syk-IN-7 (2024/9/14)
簡(jiǎn)介：syk-in-7 (compound 17) acts as an inhibitor of spleen tyrosine kinase (syk) [1].
HSP90-IN-23；化合物 HSP90-IN-23HSP90-IN-23 (2024/9/14)
簡(jiǎn)介：hsp90-in-23 (comp 12-1), a heat shock protein 90 (hsp90) inhibitor, exhibits potent activity with an ic50 of 9nm. it promotes apoptosis in tumor cells and arrests their cell cycle at the g0/g1 phase, making it applicable for cancer research [1].
Anticancer agent 130；化合物 Anticancer agent 130Anticancer agent 130 (2024/9/14)
簡(jiǎn)介：anticancer agent 130 (compound 8d) significantly induces apoptosis in a549 cells [1].
EGFR-IN-78；化合物 EGFR-IN-78EGFR-IN-78 (2024/9/14)
簡(jiǎn)介：egfr-in-78 (compound a5), a 2-aminopyrimidine derivative, serves as a reversible egfr c797s-tk inhibitor and an apoptosis inducer. it exhibits anti-proliferative properties, impedes egfr phosphorylation, and induces g2/m phase cell cycle arrest [1].
Tazarotenic acid；化合物AGN-190299AGN-190299；6-[2-(3,4-二氫-4,4-二甲基-2H-1-苯并噻喃-6-基)乙炔基]-3-吡啶甲酸|||AGN-190299 (2024/9/14)
簡(jiǎn)介：tazarotenic acid (agn-190299) is a retinoid prodrug which is converted to its active form
AChE-IN-31；化合物 AChE-IN-31AChE-IN-31 (2024/9/14)
簡(jiǎn)介：ache-in-31 (compound 1), a non-competitive acetylcholinesterase (ache) inhibitor, exhibits potential for alzheimer´s disease research [1].
H3B-968；化合物 H3B-968H3B-968 (2024/9/14)
簡(jiǎn)介：h3b-968 is a potent inhibitor of werner syndrome protein (wrn) with an ic50 of approximately 10 nm, effectively targeting its helicase, atpase, and exonuclease activities. while wrn is known for its synthetic lethal activity in cancer studies, h3b-968 specifically inhibits wrn´s helicase function through competitive atp antagonism [1].
HIF-2α-IN-9；化合物 HIF-2α-IN-9HIF-2α-IN-9 (2024/9/14)
簡(jiǎn)介：hif-2α-in-9 (compound 35r) serves as an hif-2α inhibitor, effectively suppressing vegf-a with an ic50 of 305 nm, and modulating growth-promoting genes within tumor cells while reactivating macrophage-mediated tumor immunity [1].
Antimalarial agent 27；化合物 Antimalarial agent 27Antimalarial agent 27 (2024/9/14)
簡(jiǎn)介：antimalarial agent 27 (compound 11a) potently inhibits p. falciparum with an ic50 of 0.37 μm and targets the parasite´s 1-deoxy-d-xylulose-5-phosphate reductoisomerase (dxr) enzyme with an ic50 of 0.11 μm, indicating its mechanism of action [1].
Quorum Sensing-IN-2；化合物 Quorum Sensing-IN-2Quorum Sensing-IN-2 (2024/9/14)
簡(jiǎn)介：quorum sensing-in-2 (compound 23e) is a quorum sensing inhibitor that curtails bacterial pathogenicity without impeding growth. it demonstrates minimal hemolytic activity while effectively inhibiting bacterial infections and exhibits a synergistic effect when combined with ciprofloxacin in a p. aeruginosa pao1-infected bacteremia model [1].
c-Met-IN-18；化合物 c-Met-IN-18c-Met-IN-18 (2024/9/14)
簡(jiǎn)介：c-met-in-18, an atp-competitive type-iii inhibitor, targets both wild-type (wt) and d1228v mutant c-met with ic50 values of 0.013 μm and 0.20 μm, respectively. it is utilized in research pertaining to c-met-driven cancers [1].
BD-9136；化合物 BD-9136BD-9136 (2024/9/14)
簡(jiǎn)介：bd-9136, a highly selective brd4 degrader, demonstrates the capability to inhibit tumor growth without inducing adverse effects in mice, showing potential for cancer research [1].
hDHODH-IN-12；化合物 hDHODH-IN-12hDHODH-IN-12 (2024/9/14)
簡(jiǎn)介：hdhodh-in-12 is a potent inhibitor of dihydroorotate dehydrogenase (dhodh), exhibiting an inhibitory concentration (ic50) of 0.421 μm. as the rate-limiting enzyme in the de novo synthesis of pyrimidines, critical for dna/rna synthesis, dhodh is localized within the inner membrane of human mitochondria. hdhodh-in-12 is applicable in lung cancer research [1].
SDH-IN-5；化合物 SDH-IN-5SDH-IN-5 (2024/9/14)
簡(jiǎn)介：sdh-in-5 (compound 7d), a potent inhibitor of succinate dehydrogenase (sdh) with an ic50 of 3.293 μm, additionally demonstrates antifungal efficacy, exhibiting an ec50 of 0.046 μg/ml against r. solani. moreover, sdh-in-5 significantly hampers r. solani growth in rice leaves, showcasing outstanding protective and curative effects [1].
T3SS-IN-1；化合物 T3SS-IN-1T3SS-IN-1 (2024/9/14)
簡(jiǎn)介：t3ss-in-1 (compound b9) is a potent type iii secretion system (t3ss) inhibitor that also suppresses hpa1 promoter activity and harpin protein expression, without impacting bacterial growth [1].
Bepotastine；貝托斯汀Bepotastine free base；Bepotastine free base|||貝托斯汀 (2024/9/14)
簡(jiǎn)介：bepotastine (bepotastine free base) free base is a histamine 1 (h1) receptor antagonis.
Anticancer agent 126；化合物 Anticancer agent 126Anticancer agent 126 (2024/9/14)
簡(jiǎn)介：anticancer agent 126 (compound 12), a wdr5 inhibitor, exhibits anticancer properties by disrupting the wdr5-myc interaction in cells, subsequently reducing myc target gene expression [1].
PROTAC CDK9 degrader-8；化合物 PROTAC CDK9 degrader-8PROTAC CDK9 degrader-8 (2024/9/14)
簡(jiǎn)介：protac cdk9 degrader-8 (compound 21) is a potent degrader of cdk9 with an ic50 of 0.01 μm, utilized in cancer research [1].
PSMA-IN-3；化合物 PSMA-IN-3PSMA-IN-3 (2024/9/14)
簡(jiǎn)介：psma-in-3 (compound 17) is a novel, high-affinity inhibitor of prostate-specific membrane antigen (psma) with an inhibitory concentration (ic50) of 13 nm, showing potential for the development of an 18f-labeled radioligand for positron emission tomography (pet) imaging of psma in prostate cancer [1].
SARS-CoV-2-IN-42；化合物 SARS-CoV-2-IN-42SARS-CoV-2-IN-42 (2024/9/14)
簡(jiǎn)介：sars-cov-2-in-42 (compound 8q) effectively inhibits sars-cov-2 replication with an ec50 value of 0.4 μm and demonstrates no significant toxicity to the host cell [1].
HIV-1 inhibitor-58；化合物 HIV-1 inhibitor-58HIV-1 inhibitor-58 (2024/9/14)
簡(jiǎn)介：hiv-1 inhibitor-58 (compound 10c) is a non-nucleoside reverse transcriptase inhibitor with broad-spectrum antiviral properties, effective against both wild-type strain iiib and nnrti-resistant strains like k103n and e138k in mt-4 cells at an ec50 of less than 50 nm. additionally, it inhibits cyp2c9 and cyp2c19 with ic50 values of 2.06 μm and 1.91 μm, respectively. this compound is utilized in hiv infection research [1].
TPE-1p；化合物 TPE-1pTPE-1p (2024/9/14)
簡(jiǎn)介：tpe-1p, a cascade-activated aiegen-peptide probe, self-assembles in aqueous solution to produce bright fluorescence upon interaction with alkaline phosphatase (alp) and cht-l. it facilitates noninvasive evaluation of cht-l inhibitor efficiency within cells [1].
DDO-8926；化合物 DDO-8926DDO-8926 (2024/9/14)
簡(jiǎn)介：ddo-8926 is a potent, selective bet inhibitor shown to markedly diminish mechanical hypersensitivity in neuropathic pain research by suppressing pro-inflammatory cytokine expression and decreasing neuronal excitability [1].
ARD-2051；化合物 ARD-2051ARD-2051 (2024/9/14)
簡(jiǎn)介：ard-2051 is a potent, orally active proteolysis-targeting chimera degrader of the androgen receptor (ar), exhibiting dc50 values of 0.6 nm in degrading ar protein within lncap and vcap prostate cancer cell lines. it holds potential for prostate cancer research applications [1].
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