G-5555 NEW
| Price | $48 | $68 | $89 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-07 |
Product Details
| Product Name: G-5555 | CAS No.: 1648863-90-4 |
| Purity: 99.76% | Supply Ability: 10g |
| Release date: 2024/11/07 |
Product Introduction
Bioactivity
| 名稱 | G-5555 |
| 描述 | G-5555 is a potent inhibitor of p21-activated kinase 1 (PAK1) (Kis: 3.7 nM and 11 nM for PAK1 and PAK2, respectively). |
| 體外活性 | G-5555 shows high selectivity for the group I PAKs and it also shows excellent kinase selectivity and inhibits only eight out of the 235 kinases tested other than PAK1 with inhibition >70%: PAK2, PAK3, KHS1, Lck, MST3, MST4, SIK2, and YSK1. The IC50s of G-5555 against SIK2, PAK2, KHS1, MST4, YSK1, MST3, and Lck are 9, 11, 10, 20, 34, 43, 52 nM, respectively. There is a negligible activity for G-5555 against the hERG channel with IC50 more than 10 μM in a patch-clamp assay[1]. G-5555 potently inhibits PAK2 (Ki: 11 nM). G-5555 has obviously greater growth inhibitory activity in cell lines that are PAK-amplified compared to non-amplified lines, in an array of 23 breast cancer cell lines[2]. |
| 體內(nèi)活性 | G-5555 has low blood clearance and an acceptable half-life. Good oral exposure (AUC = 30 μM?h) and high oral bioavailability (F = 80%) are achieved[1]. G-5555 inhibits phosphorylation of the PAK1/2 downstream substrate mitogen-activated protein kinase 1 (MEK1) S298, in an H292 non-small cell lunger cancer (NSCLC) xenograft study in mice. When administered at an oral dose of 25 mg/kg b.i.d., imparts 60% tumor growth inhibition in this model13 and a PAK1 amplified breast cancer xenograft model, MDAMB-175. [2] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 1 mg/ml, Sonication is recommended. |
| 關(guān)鍵字 | p21 activated kinases | PAK | G 5555 | G-5555 | Inhibitor | G5555 | inhibit |
| 相關(guān)產(chǎn)品 | Fingolimod hydrochloride | ZINC194100678 | IPA-3 | PIR 3.5 | PF-3758309 hydrochloride | FRAX1036 | FRAX597 | NVS-PAK1-1 | GNE 2861 | 5-Aminosalicylic Acid | Fingolimod | FRAX486 HCL(1232030-35-1 free base) |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 抑制劑庫 | 已知活性化合物庫 | 細(xì)胞骨架化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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