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- 上海莼试
- CS-01Y66287
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- 详细信息
- 技术资料
- 库存：
39
- 英文名：
PF-3758309
- CAS号：
898044-15-0
- 供应商：
上海莼试
- 保存条件：
Store at -20°C
- 规格：
10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg
商品属性：
产品描述：
分子式:C25H30N8OS
分子量:490.62
溶解度:≥ 24.53 mg/mL in DMSO, ≥ 101.4 mg/mL in EtOH with ultrasonic and warming
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
PF-3758309 is an inhbitor of PAK4 with IC50 of 1.3 nM [1].P21-activated kinases (PAKs) are the family of serine/theronine kinases, which play important role in linking Rho GTPase to cytoskeleton reorganization and nuclear signaling. PAK4 is a member of PAKs family, specifically responsive for interacting with GTP bound form of Cdc42 and JNK family. PAK4 is involved in filopodia formation and may play a role in the reorganization of the actin cytoskeleton.Biochemical study had identified that PF-3758309 was an ATP-competitive inhibitor of PAK4, which inhibited the kinase activity [1]. When PAK4 was screened with a panel of tumor cell lines, it was found PF-3758309 inhibited the phosphorylation of PAK4 substrate GEF-H1, and also the PAK4-induced anchorage-independent cell growth, with IC50 value of 1.3 nM and 4.7 ±3 nM respectively [1]. When PF-3758309 was screened with a panel of PAKs related kinases, it exhibited good potency and specificity for PAK4 [1]. Cell analysis con?rmed that PF-3758309 modulates PAK4-dependent signaling nodes and identi?es unexpected links to additional p53pathways [1].In vivo activity of PF-3758309 was examined in a panel of human xenograft model, including HCT116 and A549 model. Twice daily oral administration of PF-3758309 (7.5-30 mg/kg BID) for 9-18 days resulted in significant inhibition of tumor growth in all the models. The tumor growth was shown to be caused by PAK-dependent pathways in HCT116 and A549 model. Additionally, PF-3758309 was shown to regulate PAK-associated cell proliferation and survival in certain models. Therefore, PF-3758309 exhibited inhibitory activity on PAK4 [1].
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
使用方法：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
公司正在出售的产品：
| 货号 | CS-01Y66287 | 规格 | 10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg |
| CAS号 | 898044-15-0 | 分子量 | 490.62 |
| 含量 | >98.00% | 别名 | PF 3758309; PF3758309 |
| 分子式 | C25H30N8OS | 化学名 | N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-c]pyrazole-5-carboxamide |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C25H30N8OS
分子量:490.62
溶解度:≥ 24.53 mg/mL in DMSO, ≥ 101.4 mg/mL in EtOH with ultrasonic and warming
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
PF-3758309 is an inhbitor of PAK4 with IC50 of 1.3 nM [1].P21-activated kinases (PAKs) are the family of serine/theronine kinases, which play important role in linking Rho GTPase to cytoskeleton reorganization and nuclear signaling. PAK4 is a member of PAKs family, specifically responsive for interacting with GTP bound form of Cdc42 and JNK family. PAK4 is involved in filopodia formation and may play a role in the reorganization of the actin cytoskeleton.Biochemical study had identified that PF-3758309 was an ATP-competitive inhibitor of PAK4, which inhibited the kinase activity [1]. When PAK4 was screened with a panel of tumor cell lines, it was found PF-3758309 inhibited the phosphorylation of PAK4 substrate GEF-H1, and also the PAK4-induced anchorage-independent cell growth, with IC50 value of 1.3 nM and 4.7 ±3 nM respectively [1]. When PF-3758309 was screened with a panel of PAKs related kinases, it exhibited good potency and specificity for PAK4 [1]. Cell analysis con?rmed that PF-3758309 modulates PAK4-dependent signaling nodes and identi?es unexpected links to additional p53pathways [1].In vivo activity of PF-3758309 was examined in a panel of human xenograft model, including HCT116 and A549 model. Twice daily oral administration of PF-3758309 (7.5-30 mg/kg BID) for 9-18 days resulted in significant inhibition of tumor growth in all the models. The tumor growth was shown to be caused by PAK-dependent pathways in HCT116 and A549 model. Additionally, PF-3758309 was shown to regulate PAK-associated cell proliferation and survival in certain models. Therefore, PF-3758309 exhibited inhibitory activity on PAK4 [1].
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
使用方法：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
公司正在出售的产品：
| 溶质载体家族22成员18样蛋白封闭多肽 | 5-羟色胺受体1F封闭多肽 |
| TOM1L2蛋白封闭多肽 | 组蛋白去甲基化酶JMJD3抗体 |
| 前B淋巴细胞蛋白3封闭多肽 | ATP依赖解旋酶DDX19A抗体 |
| 同源转录因子DLX5封闭多肽 | 耳聋相关常染色体显性遗传5抗体 |
| 结缔组织生长因子封闭多肽 | 脂联素抗体 |
| 细胞分裂周期相关蛋白3封闭多肽 | 核苷转运蛋白ENT2抗体 |
| 死亡相关转录因子1封闭多肽 | 磷酸化Rad51抗体 |
| M-期磷蛋白6抗体封闭多肽 | 磷酸化p21蛋白抗体 |
| 黑素细胞特异性转运蛋白封闭多肽 | 磷酸化胰岛素受体底物-1抗体 |
| 磷酸化丝裂原活化蛋白激酶激酶8封闭多肽 | 腺苷酸环化酶2抗体 |
| 甲硝唑血蓝蛋白偶联物 | 细胞间粘附分子非整合素蛋白3抗体 |
| 重组人IL-7R alpha/CD127蛋白 | 精子细胞相关蛋白抗体 |
| 基质金属蛋白酶11封闭多肽 | PF-3758309神经细胞粘附分子配体1抗体 |
| 细胞外基质底物反应蛋白2封闭多肽 | 蛋白酪氨酸磷酸酶PTPLB抗体 |
| 磷酸化核因子2相关因子2(Ser40)抗体 | G21蛋白质抗体 |
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PF-3758309
￥600 - 3200
