9月
BWA-522；化合物 BWA-522BWA-522 (2024/9/14)
簡介：bwa-522 is a small molecule, orally available protein-targeting chimera (protac) that potentates the degradation of both full-length androgen receptor (ar-fl) and the ar-v7 splice variant. it specifically antagonizes the n-terminal domain (ar-ntd) of the androgen receptor (androgen receptor), prompting apoptosis in prostate cancer (pc) cells. in lncap xenograft models, bwa-522 demonstrated tumor growth inhibition (60 mg/kg, po; tgi=76%). the compound effectively reduced levels of ar-v7 and ar-fl
CTP disodium dihydrate；胞苷-5’-三磷酸二鈉鹽(二水)CTP disodium dihydrate (2024/9/14)
簡介：ctp disodium dihydrate is an agonist of p2x4 purinergic receptor
NDNA3；化合物 NDNA3NDNA3 (2024/9/14)
簡介：ndna3 (compound 14) selectively inhibits hsp90α with an ic50 of 0.51 μm, demonstrating low membrane permeability and minimal toxicity to ovcar-8 and mcf-10a cells, with ic50 values of 12.66 μm and 11.72 μm respectively. it stabilizes herg channel maturation without eliciting a heat shock response or degrading hsp90α-dependent client proteins [1].
NDNA4；化合物 NDNA4NDNA4 (2024/9/14)
簡介：ndna4 (compound 17) is a selective hsp90α inhibitor (ic50: 0.34 μm), characterized by its permanent charge and low membrane permeability. it exhibits minimal cytotoxicity against ovcar-8 and mcf-10a cell lines (ic50 >100 μm) and maintains herg channel maturation without eliciting a heat shock response or degrading hsp90α-dependent client proteins [1].
YIAD-0205；化合物 YIAD-0205YIAD-0205 (2024/9/14)
簡介：yiad-0205, an orally administered inhibitor of aβ(1-42) aggregation, has exhibited in vivo efficacy in a 5xfad transgenic mouse model that harbors five familial ad mutations [1].
PPARδ agonist 9；化合物 PPARδ agonist 9PPARδ agonist 9 (2024/9/14)
簡介：pparδ agonist 9 (compound 21), with an ec50 of 3.6 nm, is effective in vivo, decreasing serum mcp-1 concentrations in mice and markedly reducing atherosclerotic development in the ldlr-ko model with an inhibition rate of 50-60% [1].
AD4；化合物 AD4AD4 (2024/9/14)
簡介：ad4, an artemisinin derivative functioning as a proteolytic targeting chimera (protac) for pclaf, effectively degrades pclaf in rs4;11 cells with an ic50 of 0.6 nm. this degradation activates the p21/rb axis, resulting in antitumor activity. furthermore, ad4 has been demonstrated to prolong survival in nod/scid mice transplanted with rs4;11 cells, showcasing its in vivo efficacy [1].
PI3Kα-IN-12；化合物 PI3Kα-IN-12PI3Kα-IN-12 (2024/9/14)
簡介：pi3kα-in-12 (compound 13), a potent and selective pi3kα inhibitor (ic50: 1.2 nm), effectively suppresses hct-116 and u87-mg cell proliferation with ic50 values of 0.83 and 1.25 μm, respectively. intraperitoneal administration of pi3kα-in-12 (40 mg/kg) induces tumor regression in a mouse xenograft model bearing u87-mg cells [1].
SIRT5 inhibitor 7；化合物 SIRT5 inhibitor 7SIRT5 inhibitor 7 (2024/9/14)
簡介：sirt5 inhibitor 7 (compound 58), a selective and substrate-competitive sirt5 inhibitor, exhibits anti-inflammatory properties by modulating protein succinylation and attenuating pro-inflammatory cytokine release. it demonstrates renal protective effects and is active in vivo, showing efficacy in aki mouse models subjected to lipopolysaccharide (lps) and cecal ligation/perforation (clp)-induced sepsis-related acute kidney injury [1].
SIRT5 inhibitor 6；化合物 SIRT5 inhibitor 6SIRT5 inhibitor 6 (2024/9/14)
簡介：sirt5 inhibitor 6 is a potent, selective, and substrate-competitive inhibitor of sirt5, exhibiting an ic50 of 3.0 μm, and demonstrates therapeutic potential for treating septic acute kidney injury (aki) in vivo [1].
BRD7-IN-2；化合物 BRD7-IN-2BRD7-IN-2 (2024/9/14)
簡介：brd7-in-2 (compound 2-77) is a potent selective inhibitor of bromodomain-containing protein 7 (brd7), exhibiting significant anti-proliferative activity in prostate cancer cells. it demonstrates an ic50 of 5.4 μm for brd7 while showing weak inhibition for brd9 with an ic50 of >300 μm.
GST-IN-1；化合物 GST-IN-1GST-IN-1 (2024/9/14)
簡介：gst-in-1, also known as compound 16, is a potent inhibitor of glutathione s-transferase (gst), exhibiting inhibitory concentration 50 (ic50) values of 1.55 μm for sjgst and 2.02 μm for hgstm2.
IOX4；化合物IOX4IOX4 (2024/9/14)
簡介：iox4 is a potent phd2 inhibitor (ic50 = 1.6 nm)
BChE/HDAC6-IN-1；化合物 BChE/HDAC6-IN-1BChE/HDAC6-IN-1 (2024/9/14)
簡介：bche/hdac6-in-1 is a dual bche/hdac6 inhibitor that exhibits potent and selective inhibition with ic50 values of 4 nm for bche and 8.9 nm for hdac6. it demonstrates efficacy in alleviating cognitive deficits in an aβ1–42-induced mouse model, indicating its potential utility in alzheimer´s disease research [1].
MY-673；化合物 MY-673MY-673 (2024/9/14)
簡介：my-673, a colchicine binding site inhibitor (cbsi), impedes tubulin polymerization and disrupts the erk signaling pathway, consequently modulating smad4 protein expression in the tgf-β/smad pathway. this compound effectively reduces cell proliferation and migration while inducing apoptosis in both in vivo and in vitro settings [1].
FHND5071；化合物 FHND5071FHND5071 (2024/9/14)
簡介：fhnd5071, a potent and selective ret kinase inhibitor, exerts antitumor effects through the inhibition of ret autophosphorylation and may be utilized for tumor disease research [1].
MHJ-627；化合物 MHJ-627MHJ-627 (2024/9/14)
簡介：mhj-627, a potent inhibitor of erk5 (mapk7) with an ic50 value of 0.91 μm, enhances the mrna expression of tumor suppressors and anti-metastatic genes, leading to the promotion of cancer cell death [1].
IDO1/TDO-IN-6；化合物 IDO1/TDO-IN-6IDO1/TDO-IN-6 (2024/9/14)
簡介：ido1/tdo-in-6 (compound 11) is a dual inhibitor targeting ido1 and tdo, exhibiting ic50 values of 2.25 μm for ido1 and 2.89 μm for tdo. the compound further demonstrates ki values of 1.9 μm for ido1 and 3.1 μm for tdo, marking its potential utility in cancer and immunology research [1].
α-Glucosidase-IN-31；化合物 α-Glucosidase-IN-31α-Glucosidase-IN-31 (2024/9/14)
簡介：α-glucosidase-in-31 (compound r1) is a potent oral α-glucosidase inhibitor with an ic50 of 10.1 μm, demonstrating significant blood glucose reduction and antidiabetic activity [1].
MAOA-IN-1；化合物 MAOA-IN-1MAOA-IN-1 (2024/9/14)
簡介：maoa-in-1 (compound 15) is an orally-active inhibitor of monoamine oxidase a (maoa) that exhibits cytotoxic effects on prostate cancer cells. this compound demonstrates caco-2 permeability while maintaining reduced central nervous system (cns) permeability, indicating its potential utility in anti-cancer and anti-inflammatory research [1].
Multi-kinase-IN-4；化合物 Multi-kinase-IN-4Multi-kinase-IN-4 (2024/9/14)
簡介：multi-kinase-in-4 (compound 5d) is a multi-targeted kinase inhibitor active against vegfr2, egfr, her2, and cdk2, with respective ic50 values of 0.33, 0.22, 0.18, and 2.09 μm. it exhibits broad-spectrum anti-cancer properties in hepg2, mcf-7, mda-231, and hela cell lines, with ic50 values ranging from 1.94 to 7.1 μm, and demonstrates lower toxicity in wi-38 cells (ic50 = 40.85 μm). additionally, it induces apoptosis and causes s-phase cell cycle arrest in hepg2 cells, and holds potential for can
AMPK activator 12；AMPK 激活劑12AMPK activator 12 (2024/9/14)
簡介：ampk activator 12 is an ampk activator and gdf15 inducer that elevates the expression level of gdf15 protein in human hepatocytes, which can be used for cancer research.
J-1048；化合物 J-1048J-1048 (2024/9/14)
簡介：j-1048, an activin receptor-like kinase 5 (alk5) inhibitor, effectively suppresses taa-induced liver fibrosis in mice through specific inhibition of the tgf-β/smad signaling pathway [1].
TASP0415914；化合物TASP0415914TASP0415914 (2024/9/14)
簡介：tasp0415914 is an orally potent inhibitor of phosphoinositide 3-kinase γ (pi3kγ). t
hCA XII-IN-6；化合物 hCA XII-IN-6hCA XII-IN-6 (2024/9/14)
簡介：compound 4d, known as hca xii-in-6, is a potent inhibitor of human carbonic anhydrase xii (hca xii) with a ki value of 84.2 nm and exhibits anti-proliferative effects, making it useful in cancer research [1].
EGFR-IN-82；化合物 EGFR-IN-82EGFR-IN-82 (2024/9/14)
簡介：egfr-in-82 (compound 8a) is a potent, orally active inhibitor of egfr, exhibiting ic50 values of 0.09 nm for egfr l858r/t790m/c797s and 0.06 nm for egfr del19/t790m/c797s. it lacks significant inhibitory effects on egfr wt. demonstrating anti-proliferative properties, egfr-in-82 also inhibits tumor growth in nude mice, rendering it applicable in non-small cell lung cancer research [1].
PARP-1/2-IN-2；化合物 PARP-1/2-IN-2PARP-1/2-IN-2 (2024/9/14)
簡介：parp-1/2-in-2-in-1 (compound 12e) effectively inhibits parp1/2 and cdk12 with ic 50 values of 34 nm, 30 nm, and 285 nm respectively, impairing dna damage repair and inducing cell cycle arrest and apoptosis. this compound also hampers the proliferation of tnbc cells and the growth of tnbc xenograft tumors [1].
MmpL3-IN-3；化合物 MmpL3-IN-3MmpL3-IN-3 (2024/9/14)
簡介：mmpl3-in-3 (compound 12), an mmpl3 inhibitor, exhibits potent anti-tuberculosis activity with a minimum inhibitory concentration (mic) of 0.1 μm against h37rv and demonstrates good metabolic stability in mouse liver microsomes. this compound is valuable for anti-tubercular research [1].
PRDX1-IN-1；化合物 PRDX1-IN-1PRDX1-IN-1 (2024/9/14)
簡介：prdx1-in-1 is a selective inhibitor of prdx1, demonstrating an ic50 value of 0.164 μm. it is utilized in cancer research [1] due to its ability to promote intracellular ros accumulation and inhibit cancer cell proliferation, invasion, and migration while also inducing apoptosis.
RIPK3-IN-3；化合物 RIPK3-IN-3RIPK3-IN-3 (2024/9/14)
簡介：ripk3-in-3 (compound 20) is a selective ripk3 inhibitor that demonstrates potent activity with an ic50 value of 10 nm. this compound effectively blocks ripk3-mediated phosphorylation of mlkl, preventing its oligomerization and subsequent induction of necroptosis. additionally, ripk3-in-3 suppresses cxcl5 secretion and impedes aspc-1 cell migration and invasion [1].
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