W-7 hydrochloride是一种强效的钙调蛋白拮抗剂，可抑制钙离子-钙调蛋白诱导的肌球蛋白轻链激酶激活，IC50值为25μM。
Cas No.:61714-27-0
Sample solution is provided at 25 µL, 10mM.
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W-7 hydrochloride is a potent calmodulin antagonist that inhibits the Ca2+-calmodulin-induced activation of myosin light chain kinase with an IC50 value of 25μM [1]. W-7 hydrochloride enhances thromboxane A2 receptor-mediated signal transduction at the receptor/G protein coupling, leading to the enhancement of phosphoinositide hydrolysis and Ca2+ mobilization [2]. W-7 hydrochloride induces apoptosis and blocks the Akt activation[3]. W-7 hydrochloride has been widely used to inhibit peak currents of heterologously expressed Kv4.3 channels in Xenopus oocytes[4].
In vitro, W-7 hydrochloride treatment for 1h reduced colony formation of MDA-MB-231 cells with an IC50 value of 53μM[5]. Treatment with 25μM W-7 hydrochloride for 48 hours significantly inhibited the replication of Dengue virus in Huh-7 cells, reducing the secretion of NS1 protein and the expression of NS3 protein[6]. Treatment with 0.5μM W-7 hydrochloride for 24 hours significantly inhibited cytochrome c release, caspase-3 activation, reactive oxygen species (ROS) production, and cell death in PC12 cells induced by rotenone[7]. Treatment with 20μM W-7 hydrochloride for 150 minutes significantly inhibited secretion of de novo synthesized glycerolipids from McArdle RH-7777 cells[8]. Treatment with 40μM W-7 hydrochloride for 24 hours down-regulated cyclins and up-regulated p21cip1 in RPMI 8226 cells, induced cell apoptosis, accompanied by an increase in intracellular calcium ion levels and depolarization of mitochondrial membrane potential, as well as a decrease in STAT3 phosphorylation level and the reduction in Mcl-1 protein expression[9].
In vivo, W-7 hydrochloride treatment via intraperitoneal injection at a dose of 3mg/kg (5 days per week) for 18 days reduced tumor growth in RPMI 8226 cell-xenograft mouse models[9].
References:
[1] Asano M. Divergent pharmacological effects of three calmodulin antagonists, N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7), chlorpromazine and calmidazolium, on isometric tension development and myosin light chain phosphorylation in intact bovine tracheal smooth muscle[J]. The Journal of pharmacology and experimental therapeutics, 1989, 251(2): 764-773.
[2] Ohkubo S, Nakahata N, Ohizumi Y. ML-7 and W-7 facilitate thromboxane A2-mediated Ca2+ mobilization in rabbit platelets[J]. European journal of pharmacology, 1996, 298(2): 175-183.
[3] Deb T B, Coticchia C M, Dickson R B. Calmodulin-mediated activation of Akt regulates survival of c-Myc-overexpressing mouse mammary carcinoma cells[J]. Journal of Biological Chemistry, 2004, 279(37): 38903-38911.
[4] Qu Y J, Bondarenko V E, Xie C, et al. W-7 modulates Kv4. 3: pore block and Ca2+-calmodulin inhibition[J]. American Journal of Physiology-Heart and Circulatory Physiology, 2007, 292(5): H2364-H2377.
[5] Wei J W, Hickie R A, Klaassen D J. Inhibition of human breast cancer colony formation by anticalmodulin agents: trifluoperazine, W-7, and W-13[J]. Cancer chemotherapy and pharmacology, 1983, 11(2): 86-90.
[6] Bautista-Carbajal P, Soto-Acosta R, Angel-Ambrocio A H, et al. The calmodulin antagonist W-7 (N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide hydrochloride) inhibits DENV infection in Huh-7 cells[J]. Virology, 2017, 501: 188-198.
[7] Lee C S, Park S Y, Ko H H, et al. Inhibition of MPP+-induced mitochondrial damage and cell death by trifluoperazine and W-7 in PC12 cells[J]. Neurochemistry international, 2005, 46(2): 169-178.
[8] Rasouli M, Trischuk T C, Lehner R. Calmodulin antagonist W-7 inhibits de novo synthesis of cholesterol and suppresses secretion of de novo synthesized and preformed lipids from cultured hepatocytes[J]. Biochimica et Biophysica Acta (BBA)-Molecular and Cell Biology of Lipids, 2004, 1682(1-3): 92-101.
[9] Yokokura S, Yurimoto S, Matsuoka A, et al. Calmodulin antagonists induce cell cycle arrest and apoptosis in vitro and inhibit tumor growth in vivo in human multiple myeloma[J]. BMC cancer, 2014, 14(1): 882.
W-7 hydrochloride是一种强效的钙调蛋白拮抗剂，可抑制钙离子-钙调蛋白诱导的肌球蛋白轻链激酶激活，IC50值为25μM[1]。W-7 hydrochloride在受体/G蛋白偶联水平增强血栓素A2受体介导的信号转导，从而增强磷酸肌醇水解和钙离子动员[2]。W-7 hydrochloride诱导细胞凋亡，阻断Akt活化[3]。W-7 hydrochloride已被广泛用于抑制异源表达于非洲爪蟾卵母细胞中的Kv4.3通道的峰值电流[4]。
在体外，W-7 hydrochloride处理1小时降低了MDA-MB-231细胞的克隆形成能力，IC50值为53μM[5]。使用25μM的W-7 hydrochloride处理48小时，显著抑制了Dengue病毒在Huh-7细胞中的复制，降低了NS1蛋白的分泌和NS3蛋白的表达[6]。使用0.5μM的W-7 hydrochloride处理24小时，显著抑制了鱼藤酮诱导的PC12细胞中细胞色素c的释放、caspase-3的激活、活性氧（ROS）的产生以及细胞死亡[7]。使用20μM的W-7 hydrochloride处理150分钟，显著抑制了McArdle RH-7777细胞中新合成的甘油脂的分泌[8]。40μM的W-7 hydrochloride处理24小时可下调RPMI 8226细胞中的细胞周期蛋白和上调 p21cip1，诱导细胞凋亡，伴随着细胞内钙离子水平升高和线粒体膜电位去极化，以及 STAT3 磷酸化水平下降和Mcl-1蛋白表达降低[9]。
在体内，通过腹腔注射给予W-7 hydrochloride，剂量为3mg/kg（每周5天），持续18天，可抑制RPMI 8226细胞异种移植小鼠模型中的肿瘤生长[9]。
| Cell experiment [1]: | |
Cell lines | CHO-K1 cells |
Preparation Method | CHO-K1 cells were grown in Ham's F-12 medium/5% fetal calf serum at 37℃ in humidified 5% CO2/95% air; 1×104 cells were plated in 35-mm dishes and cultured for 18h. The viability of CHO-K1 cells treated with various concentrations of W-7 hydrochloride (0.1, 1, 10, and 100μM) for 48h was determined by colony formation. |
Reaction Conditions | 0.1, 1, 10, and 100μM; 48h |
Applications | W-7 hydrochloride treatment reduced cell viability of CHO-K1 in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female BALB/c nude mice |
Preparation Method | Six-week-old female BALB/c nude mice were raised under specific pathogen-free (SPF) conditions and were allowed to freely access food and tap water. 1×10⁷ RPMI 8226 cells were subcutaneously injected into the lateral abdomen of the mice. Seven days after the injection, the mice were randomly divided into two groups, with 10 mice in each group: the vehicle control group (H2O) and the W-7 hydrochloride group (dissolved in H2O). The mice were intraperitoneally injected with H2O and W-7 hydrochloride (3mg/kg) for 5 consecutive days per week for 18 days. The tumor's two-dimensional size was measured twice a week using a vernier caliper, and the tumor volume was calculated using the formula V=0.5 (a×b2), where a is the long diameter of the tumor and b is the short diameter of the tumor. |
Dosage form | 3mg/kg; 5 times a week for 18 days; i.p. |
Applications | W-7 hydrochloride treatment reduced tumor growth in murine xenograft models. |
References: | |
| Cas No. | 61714-27-0 | SDF | |
| 别名 | N-(6-氨基己基)-5-氯-1-萘磺胺盐酸盐 | ||
| 化学名 | N-(6-aminohexyl)-5-chloronaphthalene-1-sulfonamide hydrochloride | ||
| Canonical SMILES | ClC1=C2C(C(S(=O)(NCCCCCCN)=O)=CC=C2)=CC=C1.Cl | ||
| 分子式 | C16H21ClN2O2S.HCl | 分子量 | 377.33 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 14 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 0.3 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6502 mL | 13.251 mL | 26.502 mL |
| 5 mM | 530 μL | 2.6502 mL | 5.3004 mL |
| 10 mM | 265 μL | 1.3251 mL | 2.6502 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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- Purity: >98.00% Appearance: A solid
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