CS-2265
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- CAS号:
- 1652591-81-5
- 英文名:
- GSK484
- 英文别名:
- GSK484;CS-2265;AOB6992;GTPL8577;GSK484 HCl;GSK484 >=98% (HPLC);PAD4 inhibitor GS484;PAD4 inhibitor GSK484;GSK484 (hydrochloride);GSK484 hydrochloride,GSK 484,Protein Arginine Deiminase,GSK-484,GSK-484 hydrochloride,GSK484,inhibit,Peptidylarginine Deiminase,Inhibitor
- 中文名:
- CS-2265
- 中文别名:
- GSK484盐酸盐;GSK484,可逆的PAD4抑制剂;GSK485 HYDROCHLORIDE;((3S,4R)-3-氨基-4-羟基哌啶-1-基)(2-(1-(环丙基甲基)-1H-吲哚-2-基)-7-甲氧基-1-甲基-1H-苯并[D]咪唑-5-基)甲酮盐酸盐
- CBNumber:
- CB63146499
- 分子式:
- C27H32ClN5O3
- 分子量:
- 510.04
- MOL File:
- 1652591-81-5.mol
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CS-2265化学性质
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储存条件:
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2-8°C
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溶解度:
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DMSO:25.0(Max Conc. mg/mL);49.01(Max Conc. mM)
Ethanol:25.0(Max Conc. mg/mL);49.01(Max Conc. mM)
PBS buffer (pH 7.2):5.0(Max Conc. mg/mL);9.8(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);58.82(Max Conc. mM)-
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形态:
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powder
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颜色:
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white to beige
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InChIKey:
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MULKOGJHUZTANI-JEGYXLSDNA-N
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SMILES:
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C(C1CC1)N1C2=CC=CC=C2C=C1C1=NC2=CC(C(N3CC[C@@H](O)[C@@H](N)C3)=O)=CC(OC)=C2N1C.Cl |&1:22,24,r|
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CS-2265性质、用途与生产工艺
GSK484 HCl 是苯并咪唑的衍生物，是一种选择性的、可逆的 peptidylarginine deiminase 4 (PAD4) 的抑制剂，在无钙的情况下IC50值为50 nM。
| Target | Value |
PAD4
(in the absence of Calcium)
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50 nM
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GSK484 demonstrates high affinity binding to the low-calcium form of PAD4 with IC
50
s 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 NH
3
release assay.
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.
CS-2265
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/08/19 | HY-100514 | CS-2265
GSK484 hydrochloride | 1652591-81-5 | 5mg | 2100元 |
| 2024/08/19 | S7803 | CS-2265
GSK484 HCl | 1652591-81-5 | 5mg | 2574.56元 |
1652591-81-5, CS-2265 相关搜索:
- 药靶配体
- 小分子API
- 生化试剂
- 抑制剂
- C27H31N5O3ClH
- 652591-81-5
- GSK485 HYDROCHLORIDE
- GSK484,可逆的PAD4抑制剂
- ((3S,4R)-3-氨基-4-羟基哌啶-1-基)(2-(1-(环丙基甲基)-1H-吲哚-2-基)-7-甲氧基-1-甲基-1H-苯并[D]咪唑-5-基)甲酮盐酸盐
- GSK484盐酸盐
- 1652591-81-5
- GSK484 hydrochloride,GSK 484,Protein Arginine Deiminase,GSK-484,GSK-484 hydrochloride,GSK484,inhibit,Peptidylarginine Deiminase,Inhibitor
- PAD4 inhibitor GSK484
- GSK484 >=98% (HPLC)
- GTPL8577
- AOB6992
- ((3S,4R)-3-amino-4-hydroxypiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-indol-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone hydrochloride
- GSK484 HCl
- PAD4 inhibitor GS484
- CS-2265
- GSK484 (hydrochloride)
- GSK484