G-5555
Synonym(s):8-(((2r,5r)-5-Amino-1,3-dioxan-2-yl)methyl)-6-(2-chloro-4-(6-methylpyridin-2-yl)phenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one;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 NO.:1648863-90-4
- Empirical Formula: C25H25ClN6O3
- Molecular Weight: 492.96
- MDL number: MFCD28506227
- Update Date: 2026-08-30 11:39:11
What is G-5555?
Description
G-5555 is an inhibitor of p21-activated kinase 1 (PAK1; Ki = 3.7 nM), a non-receptor serine/threonine kinase involved in tumorigenesis. It is selective for PAK1 over the majority of targets in a panel of 235 kinases but does inhibit PAK2, PAK3, KHS1, LCK, MST3, MST4, SIK2, and YSK1 by greater than 70% with IC50 values ranging from 9 to 52 nM. G-5555 inhibits phosphorylation of MEK, a downstream target of PAK1, in EBC1 cells (IC50 = 69 nM). G-5555 (10, 20, and 30 mg/kg) dose-dependently reduces phosphorylation of MEK in tumors from an H292 non-small cell lung cancer (NSCLC) mouse xenograft model. G-5555 inhibits hERG channels less than 50% at a concentration of 10 μM, indicating the potential for a low risk of QT interval prolongation and potentially fatal arrhythmias.
The Uses of G-5555
G 5555 is a high affinity group 1 p21-activated kinases (PAK) inhibitor.
Storage
Store at -20°C
Properties of G-5555
| Boiling point: | 684.6±65.0 °C(Predicted) |
| Density | 1.363±0.06 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMF: 25 mg/ml; DMSO: 25 mg/ml; DMSO:PBS(pH 7.2) (1:4): 0.20 mg/ml |
| form | A crystalline solid |
| pka | 6.86±0.40(Predicted) |
| color | White to light yellow |
Safety information for G-5555
| Signal word | Warning |
| Pictogram(s) |
![]() Exclamation Mark Irritant GHS07 |
| GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
| Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for G-5555
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