9月
Glutaminase C-IN-2；化合物 Glutaminase C-IN-2Glutaminase C-IN-2 (2024/9/14)
簡介：glutaminase c-in-2 (compound 11), an allosteric inhibitor of glutaminase c (gac), exhibits potent inhibitory activity with an ic50 of 10.64 nm. by disrupting glutamine metabolism, this compound modulates cellular metabolites and elevates reactive oxygen species (ros), exerting anticancer effects [1].
SDH-IN-8；化合物 SDH-IN-8SDH-IN-8 (2024/9/14)
簡介：sdh-in-8 (compound g40) is a potent inhibitor of succinate dehydrogenase (sdh), demonstrating an ic50 value of 27 nm against porcine sdh and exhibits fungicidal properties [1].
SDH-IN-7；化合物 SDH-IN-7SDH-IN-7 (2024/9/14)
簡介：sdh-in-7 (compound g28) is a potent inhibitor of succinate dehydrogenase (sdh), exhibiting an ic50 value of 26 nm against porcine sdh and possesses fungicidal properties [1].
C25-140；化合物C25-140C25-140 (2024/9/14)
簡介：c25-140 is a small-molecule inhibitor of traf6-ubc13.
Lysyl hydroxylase 2-IN-1；化合物 Lysyl hydroxylase 2-IN-1Lysyl hydroxylase 2-IN-1 (2024/9/14)
簡介："lysyl hydroxylase 2-in-1 (compound 12) is a selective inhibitor of lysyl hydroxylase 2 (lh2) with an ic50 of approximately 300 nm and demonstrates specificity for lh2 over lh1 and lh3 [1]."
LSD1-UM-109；化合物 LSD1-UM-109LSD1-UM-109 (2024/9/14)
簡介：lsd1-um-109 is a highly potent and reversible inhibitor of lsd1, demonstrating an ic50 of 3.1 nm. this compound exhibits strong antiproliferative activity, inhibiting cell growth with ic50 values of 0.6 nm in the mv4;11 acute leukemia cell line and 1.1 nm in the h1417 small-cell lung cancer cell line [1].
ROS-IN-2；化合物 ROS-IN-2ROS-IN-2 (2024/9/14)
簡介：ros-in-2 (compound 85), a seco-lupane triterpenoid derivative, inhibits reactive oxygen species (ros) production and shields mitochondria from oxidative damage by curtailing the generation of oxidative stressors. it has applications in myocardial ischemia/reperfusion (mi/r) injury research [1].
Chitin synthase inhibitor 14；化合物 Chitin synthase inhibitor 14Chitin synthase inhibitor 14 (2024/9/14)
簡介：chitin synthase inhibitor 14 (compound 4n), a potent chitin synthase (chs) inhibitor, exhibits antifungal activity and is effective against drug-resistant fungal strains [1].
Aβ-IN-8；化合物 Aβ-IN-8Aβ-IN-8 (2024/9/14)
簡介：aβ-in-8, also known as compound 7e, is a potent inhibitor of aβ aggregation [1].
Aβ-IN-7；化合物 Aβ-IN-7Aβ-IN-7 (2024/9/14)
簡介：aβ-in-7 (compound 5a) acts as a potent inhibitor of aβ aggregation, stabilizing aβ monomers at 50 μm concentration to prevent them from forming larger oligomers and delaying the nucleation phase. comparative studies demonstrate that aβ-in-7 more effectively inhibits aβ fibril formation than aβ-in-8 at identical 50 μm concentrations [1].
DprE1-IN-9；化合物 DprE1-IN-9DprE1-IN-9 (2024/9/14)
簡介：dpre1-in-9 (compound b18) is an efficient reversible inhibitor of dpre1, interacting with the enzyme´s receptor cavity. it exhibits potent antimycobacterial properties, demonstrating activity against both non-pathogenic h37ra (mic=0.18 μg/ml) and pathogenic strains, including h37rv, as well as clinical mdr and xdr isolates [1].
NF-κB-IN-12；化合物 NF-κB-IN-12NF-κB-IN-12 (2024/9/14)
簡介：nf-κb-in-12 (compound 3h) serves as a potent inhibitor of nf-κb, exhibiting an ic50 value of 1.02 μm. it is applicable for research in acute lung injury [1].
α-Glucosidase-IN-36；化合物 α-Glucosidase-IN-36α-Glucosidase-IN-36 (2024/9/14)
簡介：α-glucosidase-in-36 (compound 5g) is a potent inhibitor of α-glucosidase, exhibiting an ic50 value of 6.69 ± 0.18 μm and inhibition constants ki and kis of 1.65 μm and 4.54 μm, respectively. it is hypothesized to suppress α-glucosidase activity by interacting with its active site and altering the enzyme´s secondary structure. the compound is relevant for use in research on type 2 diabetes mellitus (t2dm) [1].
Tubulin/HDAC-IN-3；化合物 Tubulin/HDAC-IN-3Tubulin/HDAC-IN-3 (2024/9/14)
簡介：tubulin/hdac-in-3 (compound 12a) serves as a potent dual inhibitor of tubulin polymerization and hdac1/8, exhibiting ic50 values of 5.4 μm for tubulin polymerization, and 0.155 and 0.177 μm for hdac1 and hdac8, respectively. its mechanism of action includes obstructing the cell cycle, triggering apoptosis, and suppressing colony formation [1].
Enpp-1-IN-1；化合物Enpp-1-IN-1Enpp-1-IN-1 (2024/9/14)
簡介：enpp-1-in-1 is an inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1)
CXCR4-IN-2；化合物 CXCR4-IN-2CXCR4-IN-2 (2024/9/14)
簡介：cxcr4-in-2 (compound a1), a potent bifunctional fluorinated small molecule, inhibits cxcr4 and exhibits anticancer properties by exerting cytotoxicity (ic 50: 60 μg/ml; 72 h) and antiproliferative effects on mouse colorectal cancer (crc) cells. it induces g2/m phase cell cycle arrest and apoptosis [1].
α-Amylase/α-Glucosidase-IN-5；化合物 α-Amylase/α-Glucosidase-IN-5α-Amylase/α-Glucosidase-IN-5 (2024/9/14)
簡介：α-amylase/α-glucosidase-in-5 (compound 4l) functions as a dual inhibitor, effectively inhibiting both α-glucosidase (glucosidase) and α-amylase (amylases) with ic50 values of 5.96 μm and 1.62 μm, respectively, exhibiting potential for antidiabetic activity [1].
MTX-241F；化合物 MTX-241FMTX-241F (2024/9/14)
簡介：mtx-241f, a selective small molecule inhibitor, targets members of the egfr and pi3 kinase families. it penetrates the blood-brain barrier, providing long-term tumor growth control and exhibits radiosensitizing activity in patient-derived dipg neurospheres, potentially beneficial for studying diffuse intrinsic pontine glioma (dipg) [1].
DNL343；化合物 DNL343DNL343 (2024/9/14)
簡介：dnl343, a brain-penetrating eif2b (eukaryotic initiation factor 2b) activator, suppresses the abnormal integrated stress response (isr). by inhibiting isr activity in the central nervous system (cns), dnl343 ameliorates neurodegeneration and neuroinflammation. additionally, it protects against motor dysfunction and premature death in eif2b loss-of-function (lof) mutant mice and demonstrates inhibitory potential for vanishing white matter disease (vwmd) characterized by eif2b lof and persistent i
BTM-3528；化合物 BTM-3528BTM-3528 (2024/9/14)
簡介：btm-3528 is a mitochondrial protease oma1 activator that induces an overactivation of the mitochondrial integrated stress response (isr). it promotes oma1-dependent cleavage of dele1 and opa1, leading to mitochondrial fragmentation. additionally, btm-3528 triggers eif2α kinase hri activation, resulting in cell growth arrest and apoptosis. demonstrating anticancer properties, it is effective against various dlbcl cell lines and exhibits in vivo inhibitory capabilities in a mouse model xenografted
GSK-3β inhibitor 15；化合物 GSK-3β inhibitor 15GSK-3β inhibitor 15 (2024/9/14)
簡介：gsk-3β inhibitor 15 (compound 54), with an ic50 of 3.4 nm, effectively suppresses aβ 1-42-induced phosphorylation of gsk-3β and tau protein, as well as lps-induced inos expression. it demonstrates neuroprotective properties against aβ 1-42-induced neurotoxicity, indicating its potential utility in alzheimer´s disease (ad) research [1].
CTL-12；化合物 CTL-12CTL-12 (2024/9/14)
簡介：ctl-12, a fatty acid synthase (fasn) inhibitor (ic50: 2.5 μm), induces apoptosis and disrupts the cell cycle at the sub-g1/s phase. it upregulates caspase-9 and the apoptosis marker bax, while downregulating the anti-apoptotic marker bcl-xl. by inhibiting de novo lipogenesis, ctl-12 thwarts tumor cells´ metabolic requirements and is frequently employed in breast and colorectal cancer studies [1].
CTL-06；化合物 CTL-06CTL-06 (2024/9/14)
簡介：ctl-06, a fatty acid synthase (fasn) inhibitor with an ic50 of 3 μm, induces apoptosis, while ctl-12 impedes cell cycle progression in the sub-g1/s phase and modulates apoptotic and anti-apoptotic markers by upregulating caspase-9 and bax and downregulating bcl-xl. additionally, ctl-12 suppresses de novo lipogenesis, curtailing the metabolic needs of tumor cells, with utilization in breast and colorectal cancer studies [1].
PLM-101；化合物 PLM-101PLM-101 (2024/9/14)
簡介：plm-101 is an anticancer compound orally active against acute myeloid leukemia by targeting flt3 and ret. it impedes ret function, promoting autophagic breakdown of flt3, and suppresses the pi3k and ras/erk pathways, contributing to its anti-leukemic effects. the compound´s antitumor efficacy is demonstrated in both a mouse mv4-11 flank xenograft model (doses of 3 and 10 mg/kg; po) and an allogeneic xenograft mouse model (dose of 40 mg/kg; po) [1].
TWIK-1/TREK-1-IN-3；TWIK-1/TREK-1抑制劑3TWIK-1/TREK-1-IN-3 (2024/9/14)
簡介：twik-1/trek-1-in-3 is a selective and potent inhibitor of potassium channel trek-1, inhibiting trek-1 homodimers and twik-1/trek-1 heterodimers containing two-pore-domain potassium (k2p) channels.twik-1/trek-1-in-3 exhibits antidepressant activity and can be used in the study of depression.
8-Hydroxyquinoline hemisulfate；8-羥基喹啉硫酸鹽Oxyquinoline sulfate；8-羥基喹啉硫酸鹽|||Oxyquinoline sulfate (2024/9/14)
簡介：8-hydroxyquinoline hemisulfate (oxyquinoline sulfate) is an antiseptic with mild fungistatic, bacteriostatic, anthelmintic, and amebicidal action
TWIK-1/TREK-1-IN-2；化合物 TWIK-1/TREK-1-IN-2TWIK-1/TREK-1-IN-2 (2024/9/14)
簡介：twik-1/trek-1-in-2 (compound 2g) serves as an inhibitor of both twik-1 and trek-1, targeting the trek-1 homodimer and twik-1/trek-1 heterodimer with ic50 values of 10.13 μm and 15.5 μm, respectively. additionally, it exhibits antidepressant properties [1].
TWIK-1/TREK-1-IN-1；化合物 TWIK-1/TREK-1-IN-1TWIK-1/TREK-1-IN-1 (2024/9/14)
簡介：compound 2a, identified as twik-1/trek-1-in-1, acts as an inhibitor of the trek-1, a two-pore domain potassium channel (k2p) that forms trek-1 homodimers and twik-1/trek-1 heterodimers, both significant for its role as an antidepressant target. furthermore, twik-1/trek-1-in-3, a related compound, selectively inhibits these channels with ic50 values of 9.36 μm for trek-1 homodimers and 14.6 μm for twik-1/trek-1 heterodimers, demonstrating antidepressant-like effects [1].
WU-04；化合物 WU-04WU-04 (2024/9/14)
簡介：wu-04 is a non-covalent inhibitor targeting the 3clpro protein of sars-cov-2, demonstrating high inhibitory effects on 3clpro from six sars-cov-2 variants (alpha, beta, gamma, delta, lambda, and omicron) as well as two other coronaviruses (sars-cov and mers-cov) [1].
DNA Gyrase-IN-9；化合物 DNA Gyrase-IN-9DNA Gyrase-IN-9 (2024/9/14)
簡介：dna gyrase-in-9 (compound 4j), an antibacterial agent, selectively targets dna gyrase. it exhibits a minimum inhibitory concentration (mic) of 0.5-2 μg/ml for gram-positive bacteria inhibition and a minimum bactericidal concentration (mbc) of 2-8 μg/ml for gram-positive bacteria eradication. notably, this compound hinders dna gyrase activity in staphylococcus aureus with an ic50 of 6.29 μg/ml [1].
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