G-5555
Based on 7 publication(s) in Google Scholar
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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- Purity: 99.88%
- CAS No.: 1648863-90-4
- 화학식: C25H25ClN6O3
- 분자량:492.96
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) G-5555
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Acta Pharm Sin B. 2020 Apr;10(4):603-614. [Abstract]
- Endocr Relat Cancer. 2019 Aug;26(8):699-712. [Abstract]
- PLoS One. 2024 Jul 31;19(7):e0305121. [Abstract]
- Exp Hematol. 2023 Nov:127:59-69.e2. [Abstract]
- Research Square Preprint. 2021 Apr.
- Elife. 2017 Mar 13:6:e22207. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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Flow Cytometry
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Cell Migration/Invasion Assay
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IHC
Biological Activity
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PAK1 3.7 nM (Ki) |
PAK2 11 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>1 μM
Compound: G-5555
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Growth inhibition of human A549 cells
Growth inhibition of human A549 cells
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[PMID: 28814374] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1648863-90-4
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Appearance Solid
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분자량 492.96
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화학식 C25H25ClN6O3
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Color White to light yellow
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Acta Pharm Sin B
2020 Apr;10(4):603-614. PMID: 32322465 -
Endocr Relat Cancer
2019 Aug;26(8):699-712. PMID: 31146260
G-5555 purchased from MedChemExpress. Usage Cited in: Endocr Relat Cancer. 2019 Aug;26(8):699-712. [Abstract]
A panel of eight thyroid cancer cell lines was treated with increasing doses of G-5555 or FRAX1036 for 72 hours. Cell viability was determined by colorimetric WST-8 assay.
G-5555 purchased from MedChemExpress. Usage Cited in: Endocr Relat Cancer. 2019 Aug;26(8):699-712. [Abstract]
TPC1, SW1736, K1, and FTC133 cells were treated with increasing doses of G-5555 or FRAX1036 for 24 hours to avoid significant toxicity. Western blots of downstream PAK targets were conducted to confirm drug activity.
G-5555 purchased from MedChemExpress. Usage Cited in: Endocr Relat Cancer. 2019 Aug;26(8):699-712. [Abstract]
TPC1, SW1736, and FTC133 were treated with DMSO, 0.5 μM G-5555, or 5 μM FRAX1036 for 24 or 48 hours. Cells were stained with propidium iodide and analyzed by flow cytometry for relative DNA amount.
G-5555 purchased from MedChemExpress. Usage Cited in: Endocr Relat Cancer. 2019 Aug;26(8):699-712. [Abstract]
Representative images of invading cells treated with 0.25 μM G-5555.
G-5555 purchased from MedChemExpress. Usage Cited in: Endocr Relat Cancer. 2019 Aug;26(8):699-712. [Abstract]
Representative pERK1/2 T202/Y204 IHC images showing induction of BRAFV600E in the thyrocytes with Dox treated with G-5555 (25 mg/kg, i.g.).
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PLoS One
Synergistic effect of PAK and Hippo pathway inhibitor combination in NF2-deficient Schwannoma. [Abstract]2024 Jul 31;19(7):e0305121. PMID: 39083549 -
Exp Hematol
Inhibition of PAK1 generates an ameliorative effect on MPLW515L mouse model of myeloproliferative neoplasms by regulating the differentiation and survival of the megakaryocytes. [Abstract]2023 Nov:127:59-69.e2. PMID: 37741606 -
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Elife
p27Kip1 promotes invadopodia turnover and invasion through the regulation of the PAK1/Cortactin pathway. [Abstract]2017 Mar 13:6:e22207. PMID: 28287395
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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) has not independently confirmed the accuracy of these methods. They are for reference only.
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) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (282 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Ndubaku CO, 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. [Content Brief]
[2]. Rudolph J, 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. [Content Brief]
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 |
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| 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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