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- 保存条件：
4°C, stored under nitrogen, away from moisture
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1652591-81-5
- 规格：
10 mM * 1 mL/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2356.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥2100.0 |
| 规格： | 10 mg | 产品价格： | ￥3600.0 |
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GSK484 hydrochloride
CAS No. : 1652591-81-5
MCE 国际站：GSK484 hydrochloride
产品活性：GSK484 hydrochloride 是一种有效且可逆的肽酰基精氨酸脱亚氨酶 4 (PAD4) 抑制剂。GSK484 hydrochloride 高亲和力与 PAD4 结合，在不存在钙的情况下 IC50 为 50 nM。在 2 mM 钙的存在下，IC50 为 250 nM。
研究领域：Epigenetics
作用靶点：Protein Arginine Deiminase
In Vitro: GSK484 demonstrates high affinity binding to the low-calcium form of PAD4 with IC50s of 50 nM and 250 nM in the absence of Calcium (0 mM) and Calcium (2 mM), respectively. GSK484 also inhibits PAD4 citrullination (at 0.2 mM Calcium) of benzoyl-arginine ethyl ester (BAEE) substrate in a concentration-dependent manner, as detected using an NH3 release assay.
In Vivo: 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 suppress 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, further supporting an improved functional status of the kidneys after GSK484 treatment. 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.
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文献和实验-miR-149 5,868 2,246 −1.61** 6,195 2,030 −2.05*** 6,061 1,743 −2.48*** 5,477 2,418 −1.26** hsa-miR-510 1,051 368 −1.86*** 1,489 396 −2.76*** 1,435 366 −2.92*** 1,053 384 −1.74*** hsa-miR-30a-5p 10,664
[资源] 所有的看家基因(housekeeping genes)列表+引物设计服务
sapiens replication protein A2, 32kDa (RPA2), mRNA 537 NM_004356 Homo sapiens CD81 antigen (target of antiproliferative antibody 1) (CD81), mRNA 3638 NM_001743 Homo sapiens calmodulin 2 (phosphorylase kinase, delta) (CALM2), mRNA 4675 NM_004231
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