N-[1-2(第27页)_上海陶术生物科技有限公司

T79569AChE/Aβ-IN-1；化合物 AChE/Aβ-IN-1AChE/Aβ-IN-1

AChE/Aβ-IN-1 (compound 32) is a potent, orally active acetylcholinesterase (AChE) inhibitor with an IC50 of 86 nM and an NMDA receptor antagonist targeting the GluN1-1b/GluN2B subunit combination with an IC50 of 3.876 μM. Additionally, it impedes Aβ aggregation, exhibits favorable blood-brain barrier permeability, offers neuroprotection, and enhances cognitive and spatial memory in rat models [1].

价格：￥电议型号：T79569产地：中国大陆
T79563Sirt1/2-IN-2；化合物 Sirt1/2-IN-2Sirt1/2-IN-2

Sirt1/2-IN-2 (compound hsa55) serves as a dual inhibitor for SIRT1 with an IC50 of 1.8 μM and SIRT2 with an IC50 of 2.4 μM, respectively. It effectively inhibits p53 deacetylation while enhancing the acetylation of p53 and α-tubulin. The compound also promotes apoptosis and exhibits anti-proliferative effects on human leukemia cell lines [1].

价格：￥电议型号：T79563产地：中国大陆
T79540hCA/VEGFR-2-IN-1；化合物 hCA/VEGFR-2-IN-1hCA/VEGFR-2-IN-1

hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual inhibitor targeting both Carbonic Anhydrase (CA) IX/XII and Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2). It exhibits Ki values of 4.7 nM for hCA XII and 8.3 nM for hCA IX, alongside an IC50 of 26.3 nM for VEGFR-2. This compound demonstrates anticancer activity [1].

价格：￥电议型号：T79540产地：中国大陆
T79527BET BD2-IN-1；化合物 BET BD2-IN-1BET BD2-IN-1

BET BD2-IN-1 (compound 45) is a potent, selective inhibitor of BET BD2, exhibiting an IC50 value of 1.6 nM. It suppresses Th17 cell differentiation through the reduced activation of STAT3 and NF-κB, making it relevant in research on psoriasis and inflammatory bowel disease (IBD) [1].

价格：￥电议型号：T79527产地：中国大陆
T79520HMG-CoA Reductase-IN-1；化合物 HMG-CoA Reductase-IN-1HMG-CoA Reductase-IN-1

HMG-CoA Reductase-IN-1 is an inhibitor of HMG-CoA reductase, demonstrating strong inhibitory activity on HMGR and affinity for OATP1B1, with pIC50 and pKm values of 8.54 and 1.98, respectively. It is utilized in hypercholesterolemia research [1].

价格：￥电议型号：T79520产地：中国大陆
T79514ABCG2-IN-2；化合物 ABCG2-IN-2ABCG2-IN-2

ABCG2-IN-2 is a potent inhibitor of ABCG2, exhibiting favorable oral pharmacokinetic profiles in mice, and is applicable for investigating tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP) [1].

价格：￥电议型号：T79514产地：中国大陆
T79513ABCG2-IN-1；化合物 ABCG2-IN-1ABCG2-IN-1

ABCG2-IN-1 (compound K2), an analog of Ko143, constitutes an orally active inhibitor targeting ABCG2 with an inhibitory concentration (IC50) of 0.13 μM. Demonstrating favorable oral pharmacokinetics in mice, ABCG2-IN-1 showcases promise for further research [1].

价格：￥电议型号：T79513产地：中国大陆
T79492h-NTPDase8-IN-1；h-NTPDase8 抑制剂 1h-NTPDase8-IN-1

h-NTPDase8-IN-1 is a specific aminosulfonylbenzamide inhibitor of h-NTPDases8 (IC 50 = 0.28 ± 0.07 μM). h-NTPDase8-IN-1 can be used to study diseases brought about by aberrant h -NTPDase expression.

价格：￥电议型号：T79492产地：中国大陆
T79491h-NTPDase-IN-1；化合物 h-NTPDase-IN-1h-NTPDase-IN-1

h-NTPDase-IN-1 (Compound 3i) is an inhibitor of human NTPDase (h-NTPDase) with IC50 values of 2.88 μM for h-NTPDase1 and 0.72 μM for h-NTPDase3, indicating its potential utility for thrombosis, inflammation, diabetes, and cancer research [1].

价格：￥电议型号：T79491产地：中国大陆
T79489JNK-1-IN-2；化合物 JNK-1-IN-2JNK-1-IN-2

"JNK-1-IN-2 (Compound c6) is a potent inhibitor of JNK-1 with an IC50 of 33.5 nM, and also exhibits inhibitory effects on JNK-2 and JNK-3 with IC50 values of 112.9 nM and 33.2 nM, respectively. This compound effectively inhibits the phosphorylation of c-Jun and has shown potential in reversing lung impairment, making it relevant for research into pulmonary fibrosis [1]."

价格：￥电议型号：T79489产地：中国大陆
T79488RNase L-IN-1；化合物 RNase L-IN-1RNase L-IN-1

RNase L-IN-1 (compound 17a) functions as an inhibitor of RNase L (Ribonuclease L), an enzyme responsible for RNA degradation to inhibit viral replication, and plays a crucial role in mediating innate immune responses and inflammation [1].

价格：￥电议型号：T79488产地：中国大陆
T79487MAO A/HSP90-IN-2；化合物 MAO A/HSP90-IN-2MAO A/HSP90-IN-2

MAO A/HSP90-IN-2 (compound 4-C), a dual inhibitor of HSP90 and MAO A, exhibits IC50 values of 0.016 μM for MAO A and 4.58 μM for HSP90. This compound not only enhances HSP70 expression but also diminishes HER2 and phospho-Akt levels, and downregulates IFN-γ-induced PD-L1 expression in GL26 cells. Demonstrating efficacy against Temozolomide-sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung cancer, and other malignancies, MAO A/HSP90-IN-2 may also impede tumor immune

价格：￥电议型号：T79487产地：中国大陆
T79486MAO A/HSP90-IN-1；化合物 MAO A/HSP90-IN-1MAO A/HSP90-IN-1

MAO A/HSP90-IN-1 (4-b) is a dual inhibitor of MAO A and HSP90, exhibiting IC50 values of 1.77 μM in glioblastoma (GBM) GL26 cells and 0.019 μM against HSP90α. This compound impairs the activities of MAO A, disrupts HSP90 binding, and downregulates both HER2 and phospho-Akt expressions, thereby inhibiting GBM growth. Additionally, it diminishes PD-L1 expression, thereby thwarting T cell activation and potential tumor immune evasion. MAO A/HSP90-IN-1 (4-b) is valuable for research into brain tumor

价格：￥电议型号：T79486产地：中国大陆
T79479MptpB-IN-2；化合物 MptpB-IN-2MptpB-IN-2

MptpB-IN-2 (compound 20), a selective inhibitor for mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB), exhibits half maximal inhibitory concentrations (IC50) of 0.64 μM for MptpB, 4.06 μM for MptpA, and 4.14 μM for PTP1B. Despite its inhibition potency, MptpB-IN-2 demonstrates limited antituberculosis efficacy, with a minimum inhibitory concentration (MIC) of 64.9 μM against Mtb H37Rv [1].

价格：￥电议型号：T79479产地：中国大陆
T7945917β-HSD10-IN-2；化合物 17β-HSD10-IN-217β-HSD10-IN-2

17β-HSD10-IN-2 (compound 11), a benzothiazolylurea-based inhibitor, specifically targets 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10), avoiding mitochondrial off-targets as well as cytotoxic or neurotoxic effects. This multifunctional mitochondrial enzyme inhibitor has potential applications in Alzheimer´s disease (AD) and hormone-dependent cancer research [1].

价格：￥电议型号：T79459产地：中国大陆
T79457PEX5-PEX14 PPI-IN-1；化合物 PEX5-PEX14 PPI-IN-1PEX5-PEX14 PPI-IN-1

PEX5-PEX14 PPI-IN-1 (Compound 8) is a PEX14-PEX5 protein-protein interaction (PPI) inhibitor that disrupts the interaction between PEX5 and TbPEX14 with an inhibitory constant (Ki) of 53 μM. It effectively inhibits the bloodstream form of Trypanosoma brucei brucei, with a half-maximal effective concentration (EC50) of 5 μM [1].

价格：￥电议型号：T79457产地：中国大陆
T79452Tubulin/HDAC-IN-2；化合物 Tubulin/HDAC-IN-2Tubulin/HDAC-IN-2

Tubulin/HDAC-IN-2 (Compound II-19k) is a dual inhibitor targeting Tubulin and HDAC, exhibiting IC50 values of 0.403 μM for HDAC1, 0.591 μM for HDAC2, 3.552 μM for HDAC3, and 0.459 μM for HDAC6. The compound induces G2 phase cell cycle arrest and promotes apoptosis. It effectively hampers the proliferation of both hematoma and solid tumor cells, diminishes tumor metastasis, and demonstrates tumor growth inhibition in a liver tumor allograft mouse model [1].

价格：￥电议型号：T79452产地：中国大陆
T79450Enzyme-IN-2；化合物 Enzyme-IN-2Enzyme-IN-2

Enzyme-IN-2 (compound 15) serves as a potent urease inhibitor, exhibiting anti-ureolytic activity with a K i of 2.36 ?M and an IC 50 of 0.75 ?M [1].

价格：￥电议型号：T79450产地：中国大陆
T79445KV1.3-IN-1；化合物 KV1.3-IN-1KV1.3-IN-1

KV1.3-IN-1 (Compound trans-18), a selective KV1.3 channel inhibitor with IC50 values of 230 nM in Ltk cells and 26.12 nM in PHA-activated T-lymphocytes, disrupts intracellular Ca2+ signaling and impedes T-cell activation and proliferation, as well as colony formation [1].

价格：￥电议型号：T79445产地：中国大陆
T79444HA-IN-1；化合物 HA-IN-1HA-IN-1

HA-IN-1 (compound 5g), a high-affinity Hemagglutinin (HA) ligand, targets the trypsin cleavage site of HA to inhibit HA-mediated membrane fusion and decrease pulmonary virus titer in vivo. This compound emerges as a promising influenza A virus (IAV) inhibitor and anti-influenza agent [1].

价格：￥电议型号：T79444产地：中国大陆

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