G 5555
Tocris Bioscience, part of Bio-Techne | Catalog # 6051
High affinity group I PAK inhibitor
Product Description
G 5555 is a high affinity group 1 PAK (pan-PAK1, 2 and 3) inhibitor (Ki = 3.7 nM; pMEK IC50 = 69 nM). Of 235 kinases tested, other than PAK1, eight (PAK2, PAK3, KHS1, Lck, MST3, MST4, SIK2, and YSK1) were inhibited >70%. Exhibits low hERG channel activity (<50% inhibition at 10 μM). Orally bioavailable.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of G 5555 is reviewed on the chemical probes website.
Product Specifications
Molecular Weight
492.96
Formula
C25H25ClN6O3
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
8-[(trans-5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-pyrido[2,3-d]pyrimidin-7(8H)-one
CAS Number
1648863-90-4
PubChem ID
91664373
InChI Key
ZBCMHWUFWQFPLV-UHFFFAOYSA-N
SMILES
CNC1=NC=C2C=C(C3=C(C=C(C4=CC=CC(C)=N4)C=C3)Cl)C(N(C2=N1)C[C@H]5OC[C@@H](CO5)N)=O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 49.3 | 100 | |
| DMSO | 9.86 | 20 with gentle warming |
Preparing Stock Solutions
for G 5555
The following data is based on the product molecular weight 492.96
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.03 mL | 10.14 mL | 20.29 mL |
| 5 mM | 0.41 mL | 2.03 mL | 4.06 mL |
| 10 mM | 0.20 mL | 1.01 mL | 2.03 mL |
| 50 mM | 0.04 mL | 0.20 mL | 0.41 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Ndubaku Design of selective PAK1 inhibitor G-5555: improving properties by employing an unorthodox low-pK a polar moiety. ACS Med.Chem.Lett. 2015 PMID: 26713112
Product Specific Notices for G 5555
For research use only
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