| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C26H25N5O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
BLU0588 is an orally active, potent, selective inhibitor of PRKACA (protein kinase cAMP-activated catalytic subunit alpha), with an IC50 of 1 nM and a dissociation constant (Kd) of 4 nM. It can be used for fibrolamellar carcinoma (FLC) research[1]. It is supplied as a white to yellow solid (C26H25N5O, MW 423.51) at 97.63% purity.
Physical & Chemical Properties
| CAS Number | 2810747-78-3 |
|---|---|
| Molecular Formula | C26H25N5O |
| Molecular Weight | 423.51 g/mol |
| Purity | 97.63% |
| Appearance | Solid |
| Color | White to yellow |
| SMILES | O=C(C1=CN=C(C2=C3C(NC=C3)=NC=C2)C=C1)N[C@H]4[C@H](N5CCCC5)CC6=CC=CC=C64 |
| Signaling Pathway | Stem Cell/Wnt; TGF-beta/Smad |
| Solubility | In Vitro: DMSO: 83.33 mg/mL (196.76 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 1 nM (PRKACA)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 83.33 mg/mL (196.76 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
BLU0588 (1.5 μM, 1 day or 14 days) reverses an FLC-specific gene signature: genes overexpressed in FLC (CPS1 and G6PC, top) are downregulated, whereas genes underexpressed in FLC are upregulated[1]. In FLC PDX cells, BLU0588 (0-312.5 nM) lowers pVASP in a dose-dependent manner[1].
In Vivo
BLU0588 (30-75 mg/kg, orally, once) can inhibit PRKACA and effectively blocks its downstream signaling, with phosphorylated VASP levels returning to baseline by 24 hours[1]. In mice, 30 mg/kg QD was established as the maximum tolerated dose of BLU0588 over more than 3 weeks of continuous dosing[1]. In mice, BLU0588 (30 mg/kg, orally, once daily, 34 days) can suppress tumor growth[1].
| Animal Model | female NOD-SCID mice harboring FLC PDX tumors (6-8-week-old, FLC PDX shRNA cell lines or Hep3B cells were implanted)[1] |
|---|---|
| Dosage | 30 mg/kg |
| Administration | Orally, once daily, 34 days |
| Result | Inhibited tumor growth in mice, by day 34 tumor growth was inhibited by 48.5%. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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A PKA-selective inhibitor captures an open but more ordered conformation of the PKA catalytic subunit. Proc Natl Acad Sci U S A 2026 May 12;123(19):e2536312123. PMID: 42096309
Integrative proteomic analysis reveals the cytoskeleton regulation and mitophagy difference between ischemic cardiomyopathy and dilated cardiomyopathy. Mol Cell Proteomics 2023 Dec;22(12):100667. PMID: 37852321
Genome-wide CRISPR screening reveals a PKA-driven resistance mechanism to metformin for oral cancer prevention that can be exploited by combination with NSAIDs. Cancer Prev Res 2025 Dec 19. PMID: 41416398
