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细胞周期
细胞骨架
/ PAK / G-5555

G-5555 {[allProObj[0].p_purity_real_show]}

货号：A102618

G-5555是一种选择性的 PAK1 抑制剂，Ki 值为 3.7 nM，可用于研究 PAK 相关疾病机制。

G-5555 化学结构 CAS号：1648863-90-4
G-5555 化学结构
CAS号：1648863-90-4
G-5555 3D分子结构
CAS号：1648863-90-4
G-5555 化学结构 CAS号：1648863-90-4
G-5555 3D分子结构 CAS号：1648863-90-4
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G-5555 纯度/质量文件 产品仅供科研

货号：A102618 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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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 ++++

PAK6, Ki: 17.1 nM

PAK3, IC50: 190 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。

G-5555 生物活性

描述 G-5555 is a selective PAK1 inhibitor (Ki=3.7 nM).

G-5555 细胞实验

Cell Line
Concentration Treated Time Description References
THJ-16T 2.60 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
FTC133 >10 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 had minimal effect on FTC133 cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
K1 6.98 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
8505C 6.64 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
SW1736 1.37 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
HTh74 3.36 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
BCPAP 2.46 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
TPC1 0.50 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
CMK cells 0.03, 0.1, 1, 3, 9, 20μmol/L 48 hours Inhibited CMK cell proliferation, 0.03 and 1μmol/L G5555 significantly inhibited CMK cell proliferation; 3μmol/L G5555 had a weaker inhibitory effect on CMK cell cycle; induced apoptosis, 3μmol/L G5555 increased the apoptosis rate of CMK cells by 2%. Zhonghua Xue Ye Xue Za Zhi. 2022 Jun 14;43(6):499-505
CHRF cells 0.03, 0.1, 1, 3, 9, 20μmol/L 48 hours Inhibited CHRF cell proliferation, 0.03 and 1μmol/L G5555 significantly inhibited CHRF cell proliferation; 3μmol/L G5555 reduced the percentage of CHRF cells in S phase from 37% to 15%; induced apoptosis, 3μmol/L G5555 increased the apoptosis rate of CHRF cells by 6.5%. Zhonghua Xue Ye Xue Za Zhi. 2022 Jun 14;43(6):499-505
Madin-Darby canine kidney epithelial cells 10 μM 60 minutes Measure compound permeability ACS Med Chem Lett. 2015 Oct 31;6(12):1241-6

G-5555 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Thyroid-specific inducible BRAFV600E overexpression mouse model Oral gavage 25 mg/kg Twice daily for a week To evaluate the effect of G-5555 on BRAFV600E-induced thyroid cancer, results showed that G-5555 significantly restrained thyroid size and reduced carcinoma formation Endocr Relat Cancer. 2019 Aug;26(8):699-712
Nude mice H292 NSCLC xenograft model Oral 10, 20, 30 mg/kg Single dose, tumors and blood collected 6 hours postdose Study the effect of drug dose and exposure on pharmacodynamic biomarker pMEK S298 ACS Med Chem Lett. 2015 Oct 31;6(12):1241-6

G-5555 参考文献

[1]Rudolph J, Murray LJ, et al. Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window. J Med Chem. 2016 Jun 9;59(11):5520-41.

[2]Ndubaku CO, Crawford JJ, et al. Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety. ACS Med Chem Lett. 2015 Oct 31;6(12):1241-6.

G-5555 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.14mL

2.03mL

1.01mL

20.29mL

4.06mL

2.03mL

G-5555 技术信息

CAS号1648863-90-4
分子式C25H25ClN6O3
分子量 492.96
SMILES Code ClC(C=C(C1=NC(C)=CC=C1)C=C2)=C2C3=CC4=CN=C(NC)N=C4N(C[C@@H]5OC[C@@H](N)CO5)C3=O
MDL No. MFCD28506227
别名
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

DMSO: 25 mg/mL(50.71 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: G-5555 | 1648863-90-4 | G5555 | G 5555 | PAK Inhibitor | Cell Cycle/DNA Damage | Cytoskeleton | PAK | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | G-5555 纯度/质量文件 | G-5555 亚型比较 | G-5555 生物活性 | G-5555 参考文献 | G-5555 实验方案 | G-5555 技术信息

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