cytoplasmic 1

CCR1 5 8 activator 1 是胞质磷脂酶 A 抑制剂，具有抗真菌活性。

Hydroxy-PP是一种有效的CBR1抑制剂，IC50值为0.78 μM，同时有效抑制细胞质酪氨酸激酶Fyn，IC50值为5 nM。

GSK321 是一种具有选择性和高效性的突变异柠檬酸脱氢酶 1 (IDH1) 抑制剂，抑制脂质合成并阻断 OPA1 缺陷 MEF 中的细胞增殖，可预防胞质谷氨酰胺还原羧化。GSK321 可用于研究白血病。

Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5 6 phosphorylation[1].Ipivivint (SW480 cells; 0.03 μM~3 μM; 48 hour) induced apoptosis[1]..Ipivivint (HEK-293T cells; 0.03 μM~3 μM; 1 hour) inhibits Wnt β-catenin signaling induced by Wnt3a[1].Ipivivint (SW480 cells; 0.3~10 μM; 6 hour) increases nuclear speckle enlargement[1].Ipivivint (SW480 cells; 0.3~3μM; 24hours) significantly decreases expression of Wnt target genes (AXIN2, LEF1, MYC, and TCF7) and TCF7L2. SM08502 (SW480 cells; 0.03~3μM; 24hours) inhibits cytoplasmic or nuclear fractions protein expression. Ipivivint (NCI-N87 cells) inhibits proliferation[1].Ipivivint strongly inhibits Wnt pathway signaling activity (EC50 = 0.046 μM) in SW480 colon cancer cells[1]. Ipivivint (25 mg kg; p.o.) potently inhibits tumor SRSF6 phosphorylation[1]. [1]. Tam BY, et al. The CLK inhibitor SM08502 induces anti-tumor activity and reduces Wnt pathway gene expression in gastrointestinal cancer models. Cancer Lett. 2020;473:186-197.

Thapsigargicin（Thapsigargicine）作为肥大细胞和白细胞的激活剂，能诱导大鼠腹膜肥大细胞及人嗜碱性粒细胞释放组胺，并提升完整人血小板中的细胞质游离钙水平。

Indolicidin acetate 是一种从牛中性粒细胞的细胞质颗粒中纯化的强效抗菌肽。

Protein Kinase C (19-35) Peptide 是PKC 假底物抑制剂 区域。Protein Kinase C (19-35) Peptide 阻断PKC 激酶结构域的底物结合位点，使PKC 的细胞质形式失活。

F9170是一种抗病毒肽，对应HIV-1包膜糖蛋白的789-803氨基酸。它与HIV-1包膜蛋白胞浆尾部的LLP1域结合，并抑制HIV-1 IIIB对MT-2细胞的感染(EC50 = 0.19 µM)。在恒河猴模型的类人猿免疫缺陷病毒(SHIV)感染中，F9170 (3 mg/kg)能降低血浆病毒负荷。

Gap19 是一种衍生自 Cx43 细胞质环九个氨基酸的肽，是选择性连接蛋白 43 半通道阻滞剂。它可以防止 C 末端与 CL 的分子内相互作用，具有保护心肌作用。

Cell-permeable calmodulin (CaM) agonist that binds to the EF-hand Ca2+-binding site; produces CaM-dependent activation of phosphodiesterase. Also binds to cytoplasmic sites on other Ca2+ channels, including NMDA and HIV-1 gp120-activated channels, inhibit

Antibacterialagent 144（compound 8e）是一款效能超过氯霉素和阿莫西林的抗菌药物，专门针对具有多重耐药性的金黄色葡萄球菌。该化合物通过破坏细菌的细胞质膜和抑制生物膜形成来发挥作用。Antibacterialagent 144能与HSA紧密结合（Kd=13.2 μM），显示出卓越的杀菌活性。它还能与DNA相结合，形成超分子复合物，有效阻断DNA复制过程。

HR1是一种乳突蛋白酶，可增加人红细胞膜渗透性，并能诱导细菌细胞质膜和肥大细胞质膜透化。

ICMT-IN-1 (化合物75) 作为一种高效的ICMT抑制剂展现出显著活性（IC50=0.0013 μM），能够剂量依赖性地在HCT-116细胞中导致ICMT的胞质内积累，进而有效抑制携带K-Ras和N-Ras变异的多个癌细胞系的增殖。

Z-Pro-Pro-aldehyde-dimethyl acetal 是一种高效的脯氨酸内肽酶(PRE P)抑制剂，其IC50值为12 nM。该化合物在衰老过程和神经退行性疾病，诸如阿尔茨海默病中认知功能障碍的研究中具有重要作用。

Astin C（Asterin）是一种可以从Aster tataricus中提取的天然环肽，能够特异性地阻断IRF3在STING信号体上的募集抑制cGAS-STING信号和由细胞质dna触发的先天炎症反应，导致小鼠更容易感染HSV-1，显著减弱自身炎症反应。

Gambogic amide acts as a potent and selective agonist for TrkA, promoting tyrosine phosphorylation and activating downstream signaling pathways such as Akt and MAPK. It specifically binds to the cytoplasmic juxtamembrane domain of the TrkA receptor, stimulating dimerization and activation. The compound demonstrates neuroprotective properties by preventing neuronal cell death caused by glutamate. Additionally, gambogic amide shows enhanced efficacy in a transient middle cerebral artery occlusion model of stroke and may be useful for investigating neurodegenerative diseases and stroke [1].

Dynarrestin 是一种细胞质动力蛋白 1 和 2的氨基噻唑抑制剂。它能够快速的、可逆的抑制动力蛋白 1 驱动的微管在体外滑动和细胞内动力蛋白 1 和 2 依赖性过程，且不影响 ATP 水解和干扰纤毛发生。它可抑制神经元前体和肿瘤细胞的刺猬因子依赖性增殖。

Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across isolated goby posterior intestine in 5% seawater-adapted solution.3In vivo, urotensin II (1.5-150 nmol/kg) decreases diastolic blood pressure and increases heart rate in anesthetized rats.4It also reduces the pressor responses to sympathetic nerve stimulation, norepinephrine , and vasopressin in pithed rats when administered at a dose of 150 nmol/kg. 1.Ames, R.S., Sarau, H.M., Chambers, J.K., et al.Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14Nature401(6750)282-286(1999) 2.Loretz, C.A., and Assad, J.A.Urotensin II lowers cytoplasmic free calcium concentration in goby enterocytes: Measurements using quin2Gen. Comp. Endocrinol.64(3)355-361(1986) 3.Loretz, C.A., Freel, R.W., and Bern, H.A.Specificity of response of intestinal ion transport systems to a pair of natural peptide hormone analogs: Somatostatin and urotensin IIGen. Comp. Endocrinol.52(2)198-206(1983) 4.Gibson, A., Wallace, P., and Bern, H.A.Cardiovascular effects of urotensin II in anesthetized and pithed ratsGen. Comp. Endocrinol.64(3)435-439(1986)

Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 µM, respectively). It is also active against P. falciparum, including chloroquine-susceptible and -resistant strains (IC50s = 0.85 and 0.63 µM, respectively).[2] It reduces parasitemia in a mouse model of nonlethal P. chabaudi chabaudi infection when administered at a dose of 7.5 mg/kg and increases survival in a mouse model of lethal P. chabaudi chabaudi infection. Violacein permeabilizes the cytoplasmic membrane of bacterial cells but does not affect the cell wall.[1]

Indolicidin TFA 是一种从牛中性粒细胞的细胞质颗粒中纯化的强效抗菌肽。

RyRs activator 3 (compound A4) 作为有效杀虫剂，针对斑小菜蛾 (M. separata) 及小菜蛾 (P. xylostella) 显示出较高效力，其对斑小菜蛾的 LC50 值达到 3.27 mg L。通过与兰尼碱受体 (ryanodine receptor) 结合，RyRs activator 3 能增加细胞质中 Ca2+ 的浓度，从而产生生物毒性。

RAGE 229, N-(4-(7-cyano-4-(morpholin-4ylmethyl) quinolin-2-yl)phenyl)acetamide 是一种小分子 ctRAGE-DIAPH1抑制剂，具有口服活性。RAGE 229 可通过抑制 ctRAGE 与 DIAPH1 的相互作用来抑制细胞内 RAGE 信号。

PT-129 是一种靶向 G3BP1 2 NTF2 结构域 (蛋白-RNA 相互作用位点) 的 RPOTAC 降解剂，可促进细胞内应激颗粒的分解。该化合物能抑制在应激条件下细胞内应激颗粒的形成，并作用于已存在的应激颗粒，从而干扰 ATF4 的传递，抑制癌细胞增殖。应激颗粒 (SGs) 是在应激条件下形成的无膜细胞质隔室，有助于 ATF4 从成纤维细胞迁移至肿瘤细胞，促进肿瘤生长。G3BP1 2 作为 SGs 网络的中心蛋白，其抑制作用可能降低肿瘤微环境中癌细胞的抗压能力。PT-129 由靶蛋白配体 (red part)G3BP1 2-Targeting ligand-1、E3 连接酶配体 (blue part)Thalidomide 4-fluoride 以及 PROTAC linker (black part)Amino-PEG3-C2-acid 组成；其中 E3 连接酶配体和 linker 构成复合物 Thalidomide-NH-PEG3-propionic acid。

ICMT-IN-7（化合物74）是一种高效的ICMT抑制剂，其IC50值为0.015 μM。该化合物能剂量依赖性地在HCT-116细胞中诱导ICMT蛋白在胞质的积累，并能抑制表达K-Ras和N-Ras的多种癌细胞系的增殖。