G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.
|Solubility (25°C)||DMSO 25 mg/mL|
|Storage||2-8°C, dry, sealed|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Hai-Feng Qiao, et al. J Reprod Immunol. Retraction notice to "G-5555 synergized miR-485-5p to alleviate cisplatin resistance in ovarian cancer cells via Pi3k/Akt signaling pathway" [J. Reprod. Immunol. 140C (2020) 103129]
 Roberta Tesch, et al. J Med Chem. Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors
 Hai-Feng Qiao, et al. J Reprod Immunol. G-5555 synergized miR-485-5p to alleviate cisplatin resistance in ovarian cancer cells via Pi3k/Akt signaling pathway
 Christina M Knippler, et al. Endocr Relat Cancer. MAPK- and AKT-activated thyroid cancers are sensitive to group I PAK inhibition
 Chudi O Ndubaku, et al. ACS Med Chem Lett. Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety
|Related PAK Products|
LCH-7749944 (GNF-PF-2356) is a novel and potent p21-activated kinase 4 (PAK4) inhibitor with an IC50 of 14.93 μM and has less potently inhibitory effect against PAK1, PAK5 and PAK6. LCH-7749944 causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4.
G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively.
KPT-9274, also known as PAK4-IN-1, is a potent, selective and dual PAK4/NAMPT inhibitor with IC50s of less than 100 and 120 nM, respectively.
FRAX597 is a potent, ATP-competitive inhibitor of group I PAKs with IC50 of 8 nM, 13 nM, and 19 nM for PAK1, PAK2, and PAK3, respectively.
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