GSK484盐酸盐|TQ0067|TargetMol

GSK484 hydrochloride
1652591-81-5

￥729 1mg 起订

￥1770 5mg 起订

￥2920 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: GSK484盐酸盐

英文名称：: GSK484 hydrochloride

CAS号：: 1652591-81-5

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.62%

产品类别：: 抑制剂

货号：: TQ0067

Product Introduction

Bioactivity

名称	GSK484 hydrochloride
描述	GSK484 hydrochloride (GTPL8577) is a reversible peptidyl-arginine deiminase 4 (PAD4) inhibitor. It binds to PAD4 with high affinity, with IC50 of 250 and 50 nM in the presence and absence of 2 mM calcium, respectively. GSK484 promotes the radiosensitivity of colorectal cancer (CRC) and inhibits NET formation in vitro and in vivo.
细胞实验	HEK293 cells stably expressing N-terminal FLAG-tagged PAD1, PAD2, PAD3 or PAD4 are engineered by retroviral transduction. Cells are grown in 15 cm diameter plates to subconfluency in DMEM supplemented with 10% Foetal Bovine Serum, harvested by centrifugation and washed once in PBS/2 mM EGTA. Cells are lysed in 50 mM Tris-Cl, pH 7.4, 1.5 mM MgCl2, 5% glycerol, 150 mM NaCl, 25 mM NaF, 1 mM Na3VO4, 0.4% NP40, 1 mM DTT with protease inhibitors. Lysates are pre-incubated for 20 min at 4°C with DMSO alone (2%), 100 μM of GSK199, GSK484, GSK106 or 200 μM Cl-amidine. Citrullination reactions are performed for 30 min at 37°C in the presence of 2 mM calcium. Extracts are loaded on to gels, proteins separated by SDS-PAGE and transferred to PVDF membranes. Citrullinated proteins are then chemically modified and detected using an anti-modified citrulline antibody. FLAG-PAD constructs are detected using the anti-FLAG antibody [1].
激酶实验	PAD4 is serially diluted in the presence of 10 nM GSK215 in assay buffer (100 mM HEPES, pH 8, 50 mM NaCl, 5% glycerol, 1 mM CHAPS, 1 mM DTT) at varying concentrations of calcium (0, 0.2, 2 and 10 mM). Following incubation for 50 min, apparent Kds for each calcium concentration are determined using a single site saturation curve. For IC50 determination, GSK484 is serially diluted in DMSO (1% final assay concentration) and tested at the same range of calcium concentrations in the presence of PAD4 (at the calculated Kd for each calcium condition) and 10 nM GSK215 in the same assay buffer and volume. Reactions are incubated for 50 min after which IC50 values are calculated using a four-parameter logistic equation [1].
动物实验	The study includes the MMTV-PyMT mouse model for mammary carcinoma (FVB/n background) and the RIP1-Tag2 mouse model for pancreatic neuroendocrine carcinoma (C57BL/6 background). Mice are treated daily by intra-peritoneal injections of the PAD4 inhibitor GSK484 (4 mg/kg). GSK484 is dissolved in 99.9% ethanol at a concentration of 25 mg/mL to generate a stock solution and further diluted 1:50 in 0.9% NaCl shortly before injection of 200 μL/mouse [2].
体外活性	方法：GSK484 hydrochloride (GTPL8577) （10μM）处理小鼠和人中性粒细胞，通过 Western blot 和新型成像测定证明了用钙离子载体或细菌刺激的中性粒细胞对瓜氨酸化的抑制，并进一步研究对小鼠和人中性粒细胞体外 NET 形成的影响。结果：GSK484 hydrochloride 预处理可显著减少瓜氨酸生成和 NET 形成。[1]
体内活性	To address whether PAD4 inhibition can suppress cancer-associated kidney injury, MMTV-PyMT mice are treated with the PAD4 inhibitor GSK484 at 4 mg/kg daily for one week. This dose suppresses the elevated number of neutrophils undergoing NETosis in peripheral blood in mice with cancer. In parallel, the total protein level in urine from MMTV-PyMT mice is significantly reduced compared with untreated tumor-bearing mice. Administration of GSK484 at a dose of 4 mg/kg daily during one week reverts signs of kidney dysfunction in tumor-bearing mice to the same extent as DNase I treatment, without any detectable signs of toxicity [2].
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : 100 mg/mL (196.07 mM), Sonication is recommended. PBS : <1 mg/mL (insoluble or slightly soluble) DMSO : 45 mg/mL (88.23 mM), Sonication is recommended.
关键字	GSK484 hydrochloride \| GSK 484 \| Protein Arginine Deiminase \| GTPL-8577 \| GSK484 Hydrochloride \| GTPL 8577 \| GSK-484 \| AOB-6992 \| GSK-484 hydrochloride \| GSK484 \| inhibit \| Peptidylarginine Deiminase \| GSK 484 Hydrochloride \| AOB 6992 \| Inhibitor \| GSK-484 Hydrochloride
相关产品	BMS-P5 \| BMS-P5 free base \| GSK199 \| Bongkrekic acid \| Acefylline \| GSK121 \| N-[1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide \| Cl-amidine hydrochloride
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| NO PAINS 化合物库 \| 表观遗传库

GTPL8577|||AOB6992|||GSK484盐酸盐|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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