calcium signaling

Dantrolene 是一种肌肉松弛剂，是人红细胞谷胱甘肽还原酶的非竞争性抑制剂，其Ki 和IC50值分别为 111.6 μM 和 52.3 μM。它是兰尼碱受体拮抗剂及Ca2+信号稳定剂。它可用于研究恶性高热、亨廷顿病、肌肉痉挛和其他神经阻滞剂恶性综合征。

5-(N,N-Hexamethylene)-amiloride (5-HMA) 是 amiloride 的衍生物，也是 Na+ H+交换抑制剂，可降低白血病细胞的细胞内 pH (pHi) 并诱导凋亡。

Bifenthrin 是一种合成拟除虫菊酯类杀虫剂。Bifenthrin 通过ROS生成、钙离子稳态破坏和MAPK信号级联改变诱导牛乳腺上皮细胞死亡。Bifenthrin 诱导细胞周期停滞，诱导细胞凋亡。

alpha-L-Rhamnose (6-Deoxy-L-mannose) 是存在植物和细菌中的一种单糖。Rhamnose- 免疫原连接物能被用于免疫疗法。Rhamnose 能通过胞外途径穿过上皮细胞，能够作为肠吸收的标志。

Carboxyamidotriazole Orotate (L-651582 Orotate) 是一种可口服的信号转导抑制剂，是Carboxyamidotriazole (CAI) 的乳清酸盐形式。它是一种非电压性钙通道和钙通道介导的信号通路的细胞抑制剂，具有抗癌、抗炎活性和抗血管生成作用。

Ethacrynic acid, a diuretic, functions as an inhibitor of L-type voltage-dependent and store-operated calcium channels, facilitating the relaxation of airway smooth muscle (ASM) cells. It exhibits anti-inflammatory effects, notably reducing retinoid-induced ear edema in mice, and inhibits glutathione S-transferases (GSTs), making it a potent suppressor of the NF-kB signaling pathway. Additionally, ethacrynic acid modulates leukotriene formation. A variant, Ethacrynic acid D5, is distinguished by its deuterium labeling.

Ganoderic acid F 是一种灵芝酸。它具有抗肿瘤和抗转移的活性，与抑制血管生成和涉及细胞增殖和细胞死亡，致癌作用，氧化应激，钙信号传导和内质网应激的蛋白质改变等机制相关。

Jasmonic acid (JA) 是一种植物激素，也是植物生长调节剂，参与植物迫防御和生长发育。Jasmonic acid 在信号传导过程中起着很重要的作用，诱导 MAP 激酶级联通路和钙通道发挥作用。

Carboxyamidotriazole is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling pathways. It shows anti-inflammatory, anti-tumor, and antiangiogenic effects.

ADWX 1 TFA 是一种新型肽类化合物，以1.89 pM的IC50强效抑制Kv1.3。该化合物特异性地抑制Kv1.3通道的活性，阻断初始钙信号传导和NF-κB的激活。在大鼠模型中，ADWX 1 TFA能有效改善experimental autoimmune encephalomyelitis (EAE)的症状。此外，该化合物广泛应用于研究T细胞介导的自身免疫性疾病。

BRI-50460是一种能够穿过血脑屏障的胞质钙依赖性磷脂酶A2 (cPLA2) 抑制剂，具有IC50值为0.88 nM。通过抑制cPLA2，BRI-50460调节炎症脂质信号通路，减轻淀粉样蛋白β42低聚物对cPLA2激活、tau蛋白过度磷酸化以及突触和树突减少的影响，从而发挥调节神经炎症和恢复脂质稳态的活性。此化合物适用于阿尔茨海默病及其他神经退行性疾病研究。

FLY26 是一种选择性的 GluN2B 部分拮抗剂，具有 IC50 值 0.64 μM。FLY26 通过抑制 NMDA 受体的 GluN2B 亚基来减少钙离子内流和活性氧 (ROS) 的生成，并激活 BDNF/TrkB/CREB 神经保护信号通路，从而减轻神经元兴奋性毒性和线粒体功能障碍。这使得 FLY26 在减轻脑缺血再灌注损伤引起的神经功能缺损方面有望获得应用。

Mrgx2 antagonist-3 (Compound B-40) 是一种高选择性的 MrgX2 receptor 拮抗剂，其 IC50 为 0.042-2.5 nM。它通过阻断下游 G 蛋白信号传导和 β-阻滞蛋白募集，抑制 Mrgx2 受体介导的钙内流和细胞脱颗粒。Mrgx2 antagonist-3 有潜力用于慢性荨麻疹和过敏性哮喘等炎症相关疾病和瘙痒症的研究。

Nafoxidine is a partial estrogen antagonist. It inhibits angiogenesis in some tissues by blocking the effects of VEGF and FGF; paradoxically, it may enhance angiogenesis in uterine tissue. Nafoxidine also induces calcium signaling, oxidative stress, and p

SKF-96365 hydrochloride (SKF96365) 是store-operated Ca2+entry 抑制剂，也是TRP channel 阻滞剂。它显著抑制豚鼠离体心脏 hERG、hKCNQ1/hKCNE1、hKir2.1 和 hKv4.3 电流，延长QTc 间期。它通过诱导结直肠癌细胞的细胞周期阻滞和凋亡起抗肿瘤作用。

PB28 dihydrochloride 是一种具有选择性和高效性的 sigma 2 (σ2) 受体激动剂和 σ1 受体拮抗剂，具有抗 SARS-CoV-2 活性和抗肿瘤活性，通过调节肾癌中的 PI3K-AKT-mTOR 信号通路来抑制细胞增殖和侵袭，抑制 SK-N-SH 神经母细胞瘤细胞内质网中的钙释放，可诱导非 caspase 依赖性的细胞凋亡。

GSK-A1 是 III 型磷脂酰肌醇 4-激酶 PI4KA 选择性抑制剂，pIC50为 8.5-9.8，抑制 PtdIns(4,5)P2 再合成，IC50约为 3 nM。GSK-A1有效降低 PtdIns(4)P 的水平，而对 PtdIns(4,5)P2 没影响。GSK-A1在抗丙型肝炎病毒方面有研究的潜力。

MLS1547 (MLS000051547) 是一种高效的 G 蛋白偏向多巴胺 D2 受体激动剂，Ki 为 1.2 μM。 MLS1547 在钙动员试验中刺激 D2R G 蛋白介导的信号传导，EC50 为 0.37 μM。

BM213 acetate 是一种有选择性C5aR1激动剂， 具有抗肿瘤活性，诱导 C5aR1 介导的钙动员和 pERK1/2 信号传导。

Protein kinase C (PKC ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.[1] PKC inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC .[2] It selectively and reversibly inhibits the translocation of PKC to intracellular membranes, blocking activation.[2] PKC inhibitor peptide is commonly used in cells to evaluate the role of PKC in various cellular responses.[3],[4],[5]

Protein tyrosine phosphatases (PTPs) remove phosphate from tyrosine residues of cellular proteins. Reversible phosphorylation catalyzed by the coordinated actions of protein tyrosine kinases and phosphatases is key to the regulation of the signaling events that control cell growth and proliferation, differentiation, and survival or apoptosis, as well as adhesion and motility. RK-682, a bioactive compound originally isolated from the fermentation of Streptomyces sp. 88-682, is an inhibitor of the PTPs. It inhibits the phosphorylation of CD45 and VHR with IC50 values of 54 and 2 μM, respectively, and arrests cell cycle progress at the G1/S transition. It is also reported to inhibit heparanase (IC50 = 17 μM), an endo-β-D-glucuronidase involved in tumor cell invasion and angiogenesis. RK-682 (calcium salt) is a less soluble version of the free acid.

ZQ-16是GPR84受体的高效高选择性激动剂，其EC50为0.213 μM，可激活钙离子动员、cAMP积累抑制、ERK1/2磷酸化、受体脱敏内化及β-arrestin相互作用等多条下游信号通路，是研究GPR84功能的重要工具化合物及后续优化先导物。

The phospholipases are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components. The calcium-independent phospholipases (iPLA2) are a PLA2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). Unlike (S)-BEL, (R)-BEL does not inhibit iPLA2β except at high doses of 20-30 μM. (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM.

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes. AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw. At concentrations as high as 30 μM, AX 048 does not inhibit COX activity or interfere with central cannabinoid receptor signaling.