Table 1.
Molecule | Assay readout |
EC50 (µM) |
Representative structure | Activity note | Timing (biological mode) of action |
Ref. |
---|---|---|---|---|---|---|
DMSO Butyric acid | Beating | nd | Chromatin remodeling; broadly increases transcriptional activity in cells | nd; unselective | [11] | |
Ascorbic acid | αMHC –eGFP reporter | 10.0 | Antioxidant; cosubstrate for oxoacid-dependent dioxygenases; potential signaling pathways affected include hypoxia/HIF1α and signaling by EGF repeat domain (e.g., Notch receptors) | D2–6 (not precisely determined) | [35] | |
Cardiogenols | ANF–eGFP reporter | 0.1–1 | Induces expression of GATA4 and MEF2c | <D6 (not precisely determined) | [40] | |
Isoxolyl-serines | αMHC–eGFP reporter | 10.0 | Designed as PPAR ligand but lacks PPAR agonist activity; thought to act on cardiogenesis pathways | D2–6 (not precisely determined) | [38] | |
Sulfonyl hydrazones | Nkx2.5–Luc reporter | 0.95* | Increases T/Bra+ mesoderm and possibly thereby expands the number of cardiogenic precursors | <D3 (mesoderm induction) | [33] | |
BIMR1 | αMHC–eGFP reporter | 2.34 | Unpublished | Unknown | D2–4 (mesoderm to cardiogenic mesendoderm) | Unpublished |
BIMR2 | αMHC–eGFP reporter | 1.35 | Unpublished | Unknown | D2–4 (mesoderm to cardiogenic mesendoderm) | Unpublished |
BIMR3 | αMHC–eGFP reporter | 1.75 | Unpublished | Unknown | D4–6 (cardiogenic mesoderm to cardiac tissue) | Unpublished |
Note: The table is an overview of reported synthetic cardiogenic compounds identified using HCS indicating the assay read out used, the EC50 value if available, as well as the compound’s biological mode of action, window of action, and the report reference. Timing is based on the expression of other cardiac markers as studied in the respective reports and <D6 corresponds to induction of genes such as ANF or Nkx2.5.
Abbreviations/symbols: <, before; nd, not determined;
EC50 estimated based on published data