G 5555

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Cat.No. 6051 - G 5555 | C25H25ClN6O3 | CAS No. 1648863-90-4
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

M. Wt 492.96
Formula C25H25ClN6O3
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 Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 9.86 20 with gentle warming
1eq. HCl 49.3 100

Preparing Stock Solutions

The following data is based on the product molecular weight 492.96. Batch specific molecular weights may vary from batch to batch due to solvent 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 0.2 mL 1.01 mL 2.03 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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References

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


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Keywords: G 5555, G 5555 supplier, G5555, Selective, high, affinity, group, 1, PAK, pan-PAK1, PAK2, PAK3, inhibitors, inhibits, orally, bioavailable, p21, activated, kinase, P21-activated, Kinases, 6051, Tocris Bioscience

Citations for G 5555

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