There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
规格 | 价格 | 会员价 | 库存 | 数量 | |||
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免费溶解
产品名称 | PAK ↓ ↑ | PAK1 ↓ ↑ | PAK2 ↓ ↑ | PAK3 ↓ ↑ | PAK4 ↓ ↑ | PAK5 ↓ ↑ | PAK6 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IPA-3 |
+
PAK1, IC50: 2.5 μM |
+
PAK1, IC50: 2.5 μM |
99%+ | ||||||||||||||||
FRAX486 |
+++
PAK1, IC50: 14 nM PAK4, IC50: 39 nM |
+++
PAK1, IC50: 14 nM |
++
PAK2, IC50: 33 nM |
++
PAK3, IC50: 39 nM |
+
PAK4, IC50: 575 nM |
99%+ | |||||||||||||
FRAX1036 |
++
PAK4, Ki: 23.3 nM PAK2, Ki: 72.4 nM |
++
PAK1, Ki: 23.3 nM |
++
PAK2, Ki: 72.4 nM |
+
PAK4, Ki: 2.4 μM |
99%+ | ||||||||||||||
FRAX597 |
++++
PAK2, IC50: 13 nM PAK3, IC50: 13 nM |
++++
PAK1, IC50: 8 nM |
++++
PAK2, IC50: 13 nM |
+++
PAK3, IC50: 19 nM |
98+% | ||||||||||||||
PF-3758309 |
++++
PAK3, IC50: 190 nM PAK6, Ki: 17.1 nM |
++++
PAK1, Ki: 13.7 nM |
+
PAK2, IC50: 190 nM |
++
PAK3, IC50: 99 nM |
+++
PAK4, Ki: 18.7 nM |
+++
PAK5, Ki: 18.1 nM |
+++
PAK6, Ki: 17.1 nM |
99%+ | |||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | IPA-3 inhibits Pak1 activation in part by binding covalently to the regulatory domain of Pak1. IPA-3 binds Pak1 covalently in a time- and temperature-dependent manner. IPA-3 prevents binding of the Pak1 activator Cdc42. IPA-3 binds directly to the Pak1 autoregulatory domain. IPA-3 reversibly inhibits PMA-induced membrane ruffling in cells[3]. IPA-3 (2 µM, 5 µM or 20 µM) reduces cell spreading in human primary Schwann and schwannoma cells. IPA-3 treatment significantly reduces the number of adherent Schwann and schwannoma cells in a dose-dependent manner[4]. IPA-3 prevents Cdc42-stimulated Pak1 autophosphorylation on Thr423. IPA-3 also prevents sphingosine-dependent Pak1 autophosphorylation. IPA-3 does not target exposed cysteine residues on Pak1. The disulfide bond of IPA-3 is critical for inhibition of Pak1 and in vitro reduction by the reducing agent dithiothreitol (DTT) abolishes Pak1 inhibition by IPA-3. IPA-3 inhibits activation of Pak1 by diverse activators, but does not inhibit preactivated Pak1[5]. Targeting PAK1 using IPA-3, significantly inhibits the murine metastatic PCa (RM1) cell proliferation and motility in vitro, and metastasis to the lungs in vivo[6]. Compared with spinal cord injury SCI + vehicle mice, IPA-3 treatment showed decreased p-PAK1, MMP-2, MMP-9, cleaved caspase-3, TNF-α, and IL-1β expression. Moreover, inhibition of PAK1 by IPA-3 reduced spinal cord water content and Evans blue extravasation, increased neuronal survival, and reduced TUNEL-positive cells at 24 hours after SCI[7]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
human 786-0 cell | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50=3.31805 μM | SANGER | ||
human 8305C cell | Growth inhibition assay | Inhibition of human 8305C cell growth in a cell viability assay, IC50=4.16758 μM | SANGER | ||
human A2780 cell | Growth inhibition assay | Inhibition of human A2780 cell growth in a cell viability assay, IC50=28.371 μM | SANGER | ||
human BFTC-905 cell | Growth inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=5.14768 μM | SANGER | ||
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.85mL 0.57mL 0.29mL |
14.27mL 2.85mL 1.43mL |
28.53mL 5.71mL 2.85mL |
CAS号 | 42521-82-4 |
分子式 | C20H14O2S2 |
分子量 | 350.454 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 40 mg/mL(114.14 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |