2.5-protein

MK-2461 是 ATP 竞争性的 c-Met 抑制剂, 平均 IC50 值为 2.5 nM。

Pentamidine dihydrochloride (MP-601205 dihydrochloride) 是一种抗微生物剂，会干扰 DNA 的生物合成。它是选择性蛋白酪氨酸磷酸酶和再生肝磷酸酶抑制剂。它可用于冈比亚锥虫病，抗锑利什曼病和卡氏肺孢子虫肺炎的研究，有抗肿瘤活性，抗菌活性。

STL127705 (Compound L) 是一种有效的 Ku 70 80 异二聚体蛋白抑制剂，抑制 Ku70 80-DNA 相互作用，IC50 为 3.5 μM。 它抑制 Ku 依赖性 DNA-PKCS 激酶的激活，IC50 为 2.5 μM。

LFM-A13 是一种 BTK，JAK2，PLK 有效抑制剂，可抑制 BTK、Plx1 和 PLK3 的活性，IC50分别为 2.5、10 和 61 μM。

ZIP acetate(863987-12-6 free base) 是一种新型的细胞渗透性蛋白激酶 Mζ (PKMζ) 抑制剂，它是一种参与 LTP 维持的组成型活性非典型 PKC 同工酶。在体外选择性阻断 PKMζ 诱导的海马切片突触增强。逆转晚期 LTP (IC50 = 1 - 2.5 μM) 并在体内中央给药后导致 1 天前的空间记忆持续丧失。

PTP Inhibitor IV 是一种有效的蛋白酪氨酸磷酸酶 (PTP) 抑制剂，可选择性抑制 DUSP14 磷酸酶活性（IC50 ： 5.21 μM）。PTP Inhibitor IV 对 SHP-2、PTP1B、PTP-ε、PTP Meg-2、PTP-σ、PTP-β 和 PTP-μ具有抑制作用，IC50 分别为 1.8 μM、2.5 μM、8.4 μM、13 μM、20 μM、6.4 μM，和 6.7 μM。PTP Inhibitor IV 通过抑制PTP 活性，影响细胞信号传导，并可能调节与PTP 介导的信号传导事件相关的特定途径。

Novel, cell-permeable inhibitor of protein kinase Mζ (PKMζ), a constitutively active, atypical PKC isozyme involved in LTP maintenance. Selectively blocks PKMζ-induced synaptic potentiation in hippocampal slices in vitro. Reverses late-phase LTP (IC50 = 1

ML266 是葡萄糖脑苷脂酶 (GCase) 分子伴侣， IC50值为 2.5 µM。ML266与 GCase 结合并将其转运至溶酶体，恢复 GCase 酶的活性。ML266 不会抑制 GCase 的活性。ML266 具有研究戈谢病的潜力。

DC-CPin7, a powerful inhibitor of the bromodomain of CREB-binding protein (CBP), exhibits an IC50 value of 2.5 μM [1].

Quinacrine is a compound with multiple actions that is commonly used as an anti-protozoal agent. It has also been shown to be a highly potent autophagy inhibitor, although the dose required to achieve this effect is considerably cytotoxic (LD50 = 2.5 μM). Quinacrine analog 34 is a derivative of quinacrine that was designed with an improved cell viability profile (LD50 = 27 μM) to inhibit autophagy. At a minimum concentration of 0.5 μM, this compound has been shown to increase the protein levels of the autophagy biomarker LC3-II and to induce lysosome deacidification.

Protein kinase D (PKD), a serine threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.

mSIRK (G-Protein βγ Binding Peptide) 是一种细胞渗透性 ERK1 和 ERK2 双重激活剂，是一种由15个氨基酸组成的多肽，可促进α亚基解离。

Dendrogenin A (DDA) 作为一种选择性肝X受体(LXR)调节剂(SLiM)、胆固醇环氧水解酶(ChEH; Ki = 120 nM)的抑制剂及胆固醇的活性代谢产物，通过DDA合成酶将5,6α-环氧胆固醇与组胺结合形成。DDA在非癌性人乳腺上皮细胞和上皮黑色素细胞中存在，但在多种乳腺癌细胞或黑色素瘤细胞中未发现，且在分离的人乳腺肿瘤组织中仅以低水平存在。它抑制22(R)-羟基胆固醇诱导的LXRβ和LXRα激活(分别以IC50 = 76和362 nM)，但也是LXR的部分激动剂，在B16/F10小鼠黑色素瘤细胞中增加Nur77、NOR-1、LC3-I和LC3-II的蛋白水平。DDA选择性调节LXRα和LXRβ，而非孕烯X受体(PXR)、芳香烃受体(AhR)、维生素D受体(VDR)、维甲酸X受体γ(RXRγ)、维甲酸受体α(RARα)、过氧化物酶体增殖物激活受体α(PPARα)、PPARγ、糖皮质激素受体、雄激素受体、雌激素受体α(ERα)及ERβ在2.5 µM下。此外，DDA在2.5和5 µM的浓度下增加B16/F10和SK-MEL-28癌细胞中LC3-II的蛋白水平，并在2.5 µM时诱导这些细胞类型的自噬细胞死亡。DDA (0.37 µg/kg)在B16/F10小鼠黑色素瘤模型和TS/A小鼠乳腺癌模型中减缓肿瘤生长，并在体内外诱导癌细胞分化。

YW3-56 is an inhibitor of protein arginine deiminase 2 (PAD2) and PAD4 (IC50s = 0.5-1 and 1-5 μM, respectively).1It inhibits the growth of U2OS osteosarcoma cells (IC50= ~2.5 μM) in a p53-dependent mannerviainduction of SESN2 and subsequent inhibition of mTORC1. YW3-56 (10 mg kg) reduces tumor growth in an S-180 murine sarcoma tumor model. It also inhibits tumor growth in the 1883 MDA-MB-231 breast cancer bone metastasis mouse xenograft model.2 1.Wang, Y., Li, P., Wang, S., et al.Anticancer peptidylarginine deiminase (PAD) inhibitors regulate the autophagy flux and the mammalian target of rapamycin complex 1 activityThe Journal of Biological Chemisty287(31)25941-25952(2012) 2.Wang, S., Chen, X.A., Hu, J., et al.ATF4 gene network mediates cellular response to the anticancer PAD inhibitor YW3-56 in triple-negative breast cancer cellsMol. Cancer Ther.14(4)877-888(2015)

Blapsin B is a potent 14-3-3 inhibitor. Blapsin B is a naturally occurring compound isolated from the ethanol extract of the stink beetle, Blaps japanensis. Blapsin B potently inhibited 14-3-3 protein-protein interactions (PPIs) with IC(50) value of 10.0 μM as determined by an ELISA assay, and 2.5 μM in an FP assay, respectively. Blapsin B represent the first example of natural small-molecule 14-3-3 inhibitors.

EMT inhibitor-3 (compound 11i) 是一种能够抑制上皮-间质转化 (EMT) 的化合物，对神经母细胞瘤 SK-N-SH 细胞的抑制IC50值为2.5 μM。它可抑制SK-N-SH细胞的增殖、迁移和侵袭，通过增加Bax Bcl-2蛋白表达比例促进细胞色素 (Cytochrome C) 从线粒体释放，并激活caspase 9和caspase 3，从而诱导线粒体介导的内源性细胞凋亡 (Apoptosis)。EMT inhibitor-3 可用于癌症研究。

icFSP1是一种抑制剂，针对的是铁死亡抑制蛋白1（FSP1）。在2.5 µM的浓度下使用时，能够引发FSP1在细胞中的凝聚和相分离，但在无细胞测试中并不抑制FSP1的酶活性（IC50 = > 30 µM）。icFSP1以浓度依赖的方式诱导HT-1080纤维肉瘤细胞的铁死亡。在体内，icFSP1（50 mg kg）通过使用人类过表达FSP1，Gpx4- -Fsp1- -的B16 F10细胞，在B16 F10鼠黑色素瘤模型中减少肿瘤体积和重量。

Antimycobacterial agent-8 (Compound 49) 作为 DNA gyrase 的抑制剂,在抗菌领域显示出显著效果.其对 Mycobacterium tuberculosis 和 M. abscessus 的最小抑制浓度(MIC90)分别为2.5 μM 和 0.63 μM.此外,该化合物在小鼠体内显示出优秀的血浆蛋白结合性能.

CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1]. In cultured C2C12 myotubes, CC260 (20 μM) enhances Insulin-induced Akt phosphorylation at both Thr-308 and Ser-473 but suppresses S6K phosphorylation (Thr-389) by mTORC1[1]. CC260 (2.5 μM, 5 μM, 10 μM, 20 μM) significantly increases phosphorylation of acetyl-CoA carboxylase (ACC) in a dose-dependent manner[1]. CC260 treatment reduces the ability of BT474 cells to survive serum starvation, which could be rescued by expressing the PI5P4Kβ refractory mutant[1]. In BT474 cells, CC260 treatment causes an increase in glycolytic ATP production[1]. [1]. Song Chen, et al. Pharmacological inhibition of PI5P4Kα β disrupts cell energy metabolism and selectively kills p53- tumor cells. Proc Natl Acad Sci U S A. 2021 May 25;118(21):e2002486118.

2-Chloroadenosine 5-triphosphate (2-chloro ATP), an analog of ATP and adenine nucleotide, functions as an antagonist of the purinergic P2Y1 receptor, inhibiting ADP-induced intracellular calcium mobilization in Jurkat cells with a Ki value of 2.3 µM. Additionally, 2-chloro ATP acts as an agonist of purinergic P2X receptors, demonstrated by inducing inward currents in HEK293 cells expressing either human bladder smooth muscle or rat PC12 receptor forms, with EC50 values of 0.5 and 2.5 µM, respectively. It also triggers relaxation in precontracted isolated guinea pig taenia caeci strips in a concentration-dependent fashion. Furthermore, 2-chloro ATP has been employed in research to investigate the substrate specificity of cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and PKG.

Keap1-Nrf2-IN-3 is a KEAP1:NRF2 protein protein interaction inhibitor, and with a K d value of 2.5 nM for KEAP1 protein.

Keap1-Nrf2-IN-15 (Compound 24a) 作为Keap1-Nrf2蛋白-蛋白相互作用抑制剂，其FP试验与TR-FRET试验的IC50值分别为77 nM和2.5 nM，显示出高效的抑制活性。

TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistically with gemcitabine to reduce the viability of HPAC cells. 1.Zhang, X., Zegar, T., Weiser, T., et al.Characterization of a dual BET HDAC inhibitor for treatment of pancreatic ductal adenocarcinomaInt. J. Cancer147(10)2847-2861(2020)