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Pathway Inhibitors

GW296115X View larger

GW296115X

AOB4180

CAS 118458-58-5

Chemical Name: 3744W; 12,13-Dihydro-3,9-dimethoxy-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione

AOBIOUS launched this product in 2022

CITATIONS - Publications That Use AOBIOUS Product

1) Front. Cell. Infect. Microbiol., 24 March 2024

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$89.00

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QuantitymgUnit Price ($/mg or $/Unit)Final Price
15 $75.65 Total: $378.25
110 $64.08 Total: $640.80
125 $54.29 Total: $1,357.25
150 $46.28 Total: $2,314.00
1100 $40.05 Total: $4,005.00

Data sheet

Molecular FormulaC22H15N3O4
Molecular Weight385.37
CAS Numbers118458-58-5
Storage Condition0°C (short term), -20°C (long term), desiccated
SolubilityDMSO
Purity98% by HPLC
Synonym3744W
IUPAC/Chemical Name12,13-Dihydro-3,9-dimethoxy-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione
InChl KeyLGTURXDQKJRHSF-UHFFFAOYSA-N
InChl CodeInChI=1S/C22H15N3O4/c1-28-9-3-5-13-11(7-9)15-17-18(22(27)25-21(17)26)16-12-8-10(29-2)4-6-14(12)24-20(16)19(15)23-13/h3-8,23-24H,1-2H3,(H,25,26,27)
SMILES CodeCOC1=CC2=C(C=C1)NC3=C4C(=C5C(=C23)C(=O)NC5=O)C6=C(N4)C=CC(=C6)OC

More info

Potent, selective inhibitor of human cytomegalovirus replication; Inhibitor of the autophosphorylation of the cytoplasmic domain both in vitro and within intact insect cells

Mechanism / Targets

  • GW296115X is an indolocarbazole-type small molecule. PubMed+4ZFIN+4ASM Journals+4

  • It functions as a kinase inhibitor, especially of lesser-studied (“dark”) kinases. For example, it inhibits BRSK2 (and BRSK1) with low nanomolar potency in biochemical assays. ResearchGate+2ZFIN+2

  • It also inhibits receptor tyrosine kinase autophosphorylation (e.g., PDGF-dependent receptor autophosphorylation) and cell proliferation. ZFIN+1

  • In the context of intracellular bacterial infection (e.g., Methicillin‑resistant Staphylococcus aureus / MRSA), GW296115X appears to activate the cellular energy-sensor kinase AMPK (via increased phosphorylation of AMPK Thr172), induce autophagy (increased LC3-II / LC3-I ratio) and thereby promote degradation of intracellular bacteria. Frontiers+2PubMed+2

Functional activities in cellular/infection models

  • In a study screening for host-directed therapy (HDT) against intracellular MRSA, GW296115X reduced the intracellular bacterial burden in HeLa cells by up to ~80% (IC₅₀ ~159 nM) without significantly impairing host cell viability at effective concentrations. Frontiers+2PubMed+2

  • It synergized with standard antibiotics (e.g., Vancomycin, Daptomycin) to enhance clearance of intracellular and extracellular MRSA. PubMed+1

  • In another infection model (screening of kinase inhibitors in intracellular bacterial infections), it showed efficacy in HeLa cells but reduced activity in primary macrophages under certain conditions. Nature+1

Summary 

  • GW296115X acts as a chemical probe/kinase inhibitor (especially BRSK2) with cellular activity.

  • It induces AMPK activation and autophagy in host cells, altering host-cell signalling rather than directly killing bacteria (for the MRSA model).

  • It is being explored as a host-directed therapeutic (HDT) agent rather than a classical antibiotic.

  • It may serve as a tool compound to interrogate understudied kinase functions and host-pathogen interactions.