G 5555

Pricing Availability   Qty
Description: High affinity group I PAK inhibitor
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
Purity: ≥98% (HPLC)
Citations (1)

Biological Activity for G 5555

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.

Technical Data for G 5555

M. Wt 492.96
Formula C25H25ClN6O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1648863-90-4
PubChem ID 91664373
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for G 5555

Solvent Max Conc. mg/mL Max Conc. mM
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 will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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 0.2 mL 1.01 mL 2.03 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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References for G 5555

References are publications that support the biological activity of the product.

Ndubaku et al (2015) Design of selective PAK1 inhibitor G-5555: improving properties by employing an unorthodox low-pK a polar moiety. ACS Med.Chem.Lett. 6 1241 PMID: 26713112

If you know of a relevant reference for G 5555, please let us know.

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1 Citation for G 5555

Citations are publications that use Tocris products. Selected citations for G 5555 include:

Teresa L et al (2021) PAK1 Positively Regulates Oligodendrocyte Morphology and Myelination. J Neurosci 41 1864-1877 PMID: 33478987

Do you know of a great paper that uses G 5555 from Tocris? Please let us know.

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