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SML3237

G-5555

≥98% (HPLC)

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

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About This Item

Empirical Formula (Hill Notation):
C25H25ClN6O3
CAS Number:
1648863-90-4
Molecular Weight:
492.96
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD28506227
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/L, clear

storage temp.

−20°C

General description

G-5555 is a selective p21-activated kinase (PAK1) inhibitor. In addition to this it also selectively inhibits eight kinases such as PAK2, PAK3, KHS1, lymphocyte-specific protein tyrosine kinase (LcK), Mammalian Ste20-like kinase 3 (MST3), Mammalian Ste20-like kinase 4 (MST4), salt-inducible kinase 2(SIK2), and Yeast Sps1/Ste20-related Kinase 1 (YSK1). G-5555 exhibits high stability and low human ether-à-go-go related gene (hERG) activity than other PAK inhibitors including FRAX1036.[1]

Biochem/physiol Actions

ATP site-targeting inhibitor against SIK1/2/3, MST3/4, PAK1/2, YANK1/3, MAP2K5 and MAP4K5. Reduces cellular MEK pS298 in cultures and in mice in vivo.
G-5555 is an ATP site-targeting inhibitor against salt-inducible kinases, MST3/4, p21-activated kinase 1/2, YANK1/3, MAP2K5, MAP4K5 (% inhibition at 100 nM = 98.6/93.5/99.8 (SIK1/2/3), 85/99.5 (MST3/4), 95.6/87 (PAK1/2), 94.7/96.5 (YANK1/3); 87/MAP2K5, 83/MAP4K5) with good selectivity over other kinases. G-5555 downregulates MEK pS298 in EBC1 cells in cultures (IC50 = 69 nM) and in H292 NSCLC tumors in mice in vivo (25 mg/kg p.o.) with good oral availability (mice F = 80%, monkeys F = 72%).
G-5555 is an ATP site-targeting inhibitor against salt-inducible kinases, MST3/4, p21-activated kinase 1/2, YANK1/3, MAP2K5, MAP4K5 (% inhibition at 100 nM = 98.6/93.5/99.8 (SIK1/2/3), 85/99.5 (MST3/4), 95.6/87 (PAK1/2), 94.7/96.5 (YANK1/3); 87/MAP2K5, 83/MAP4K5) with good selectivity over other kinases. G-5555 downregulates MEK pS298 in EBC1 cells in cultures (IC50 = 69 nM) and in H292 NSCLC tumors in mice in vivo (25 mg/kg p.o.) with good oral availability (mice F = 80%, monkeys F = 72%). PAK1 plays a crucial role in cancer progression, inhibiting this protein has the potential to reduce cancer development. Therefore, G-5555 may be a promising candidate for oncology research.

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G-5555 ≥98% (HPLC)

Sigma-Aldrich

SML3237

G-5555

GSK1838705A ≥98% (HPLC)

Sigma-Aldrich

SML0995

GSK1838705A

GNE-317 ≥98% (HPLC)

Sigma-Aldrich

SML3363

GNE-317

LY3009120 ≥98% (HPLC)

Sigma-Aldrich

SML3055

LY3009120

form

powder

form

powder

form

powder

form

powder

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

storage temp.

2-8°C

solubility

DMSO: 2 mg/L, clear

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear (warmed)

color

white to beige

color

white to light brown

color

white to beige

color

white to beige

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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