2. Cell Cycle/DNA Damage Cytoskeleton
  3. PAK
  4. G-5555

G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.

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G-5555

G-5555 構造式

CAS 番号 : 1648863-90-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 119 在庫あり
Solution
10 mM * 1 mL in DMSO USD 119 在庫あり
Solid
1 mg $70 在庫あり
5 mg $110 在庫あり
10 mg $160 在庫あり
25 mg $360 在庫あり
50 mg $640 在庫あり
100 mg $1100 在庫あり
250 mg $1650 在庫あり
500 mg $2250 在庫あり
1 g $2950 在庫あり
5 g   お問い合わせ  
10 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 7 publication(s) in Google Scholar

Other Forms of G-5555:

G-5555 関連抗体

Top Publications Citing Use of Products

PAK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.

IC50 & Target[2]

PAK1

3.7 nM (Ki)

PAK2

11 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 1 μM
Compound: G-5555
Growth inhibition of human A549 cells
Growth inhibition of human A549 cells
[PMID: 28814374]
体外実験

G-5555 is a potent PAK1 inhibitor with a Ki of 3.7 nM. G-5555 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. In general, G-5555 demonstrates high selectivity for the group I PAKs. There is 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, with a Ki of 11 nM. In an array of 23 breast cancer cell lines, G-5555 has significantly greater growth inhibitory activity in cell lines that are PAK-amplified compared to non-amplified lines[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

G-5555 関連抗体
体内実験

G-5555 exhibits low blood clearance and an acceptable half-life. Good oral exposure (AUC = 30 μM h) and high oral bioavailability (F = 80%) are achieved[1]. In an H292 non-small cell lunger cancer (NSCLC) xenograft study in mice, G-5555 inhibits phosphorylation of the PAK1/2 downstream substrate mitogen-activated protein kinase 1 (MEK1) S298 and, when administered at an oral dose of 25 mg/kg b.i.d., imparts 60% tumor growth inhibition in this model and a PAK1 amplified breast cancer xenograft model, MDAMB-175[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

492.96

分子式

C25H25ClN6O3
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外: 

DMSO : 25 mg/mL (50.71 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0286 mL 10.1428 mL 20.2856 mL
5 mM 0.4057 mL 2.0286 mL 4.0571 mL
10 mM 0.2029 mL 1.0143 mL 2.0286 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.88%

COA (254 KB) LCMS (102 KB)

取扱説明書 (2659 KB)
参考文献
キナーゼ実験
[1]

The 10 µL assay mixtures contain 50 mM HEPES (pH 7.5), 0.01% Brij-35, 10 mM MgCl2, 1 mM EGTA, 2 µM FRET peptide substrate, and PAK enzyme (20 pM PAK1; 50 pM PAK2; 90 pM PAK4). Incubations are carried out at 22°C in black polypropylene 384-well plates. Prior to the assay, enzyme, FRET peptide substrate and serially diluted test compounds (G-5555, etc.) are preincubated together in assay buffer (7.5 µL) for 10 minutes, and the assay is initiated by the addition of 2.5 µL assay buffer containing 4× ATP (160 µM PAK1; 480 µM PAK2; 16 µM PAK4). Following the 60-minute incubation, the assay mixtures are quenched by the addition of development reagent, and 1 hour later the emissions of Coumarin (445 nm) and Fluorescein (520 nm) are determined after excitation at 400 nm[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[1]

Mice[1]
Three mice in each of the two groups are administered 25 mg/kg oral suspension dose twice, with the second dose given 6 hours after the first dose. The dose volumes are 5 mL/kg for the IV group and 10 mL/kg for the PO groups. Following administration of G-5555, 15 µL of blood is collected at each time point are stored at -70 to -80°C until analysis[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0286 mL 10.1428 mL 20.2856 mL 50.7141 mL
5 mM 0.4057 mL 2.0286 mL 4.0571 mL 10.1428 mL
10 mM 0.2029 mL 1.0143 mL 2.0286 mL 5.0714 mL
15 mM 0.1352 mL 0.6762 mL 1.3524 mL 3.3809 mL
20 mM 0.1014 mL 0.5071 mL 1.0143 mL 2.5357 mL
25 mM 0.0811 mL 0.4057 mL 0.8114 mL 2.0286 mL
30 mM 0.0676 mL 0.3381 mL 0.6762 mL 1.6905 mL
40 mM 0.0507 mL 0.2536 mL 0.5071 mL 1.2679 mL
50 mM 0.0406 mL 0.2029 mL 0.4057 mL 1.0143 mL
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G-5555 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

G-55551648863-90-4G5555G 5555PAKp21 activated kinasesInhibitorinhibitorinhibit

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製品名:
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製品番号:
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