G 5555

Name: G 5555
Brand: Tocris Bioscience
SKU: 6051

Tocris Bioscience, part of Bio-Techne | Catalog # 6051

Citations (3)

COA / SDS

High affinity group I PAK inhibitor

Key Product Details

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)
Molecular Weight:	492.96

View Full Technical Details for G 5555

Technical Data
Citations

Biological Activity for G 5555

G 5555 is a high affinity group 1 PAK (pan-PAK1, 2 and 3) inhibitor (K_i = 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	C₂₅H_25ClN₆O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
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.

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

Solubility for G 5555

	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 will 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

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References for G 5555

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