Table 3.

Inhibitors targeting m¹A-related regulators.

Target	Compound	Mechanism	Effect on cancer
TRMT6/TRMT61A	Thiram	Inhibits TRMT6-TRMT61A interaction	HCC: Suppress self-renewal and tumor growth [62]
ALKBH3	HUHS015/Compound 7I	Suppress ALKBH3 activity	PC: Inhibit proliferation of DU145 cells [83], [84]
FTO	18077/18097	Bind to the active site of FTO	BC: Inhibited cell cycle process and migration of cancer cells [86]
	CHTB	Bind to a novel site of FTO and inhibit demethylase activity [89]	−
	CS1/CS2	Block the catalytic pocket of FTO	AML: Inhibits cancer cell proliferation, cancer stem cell self-renewal and immune evasion [90]
	Dac51	Suppress FTO activity	Melanoma: Promotes T cell response and enhances the anti-PD-1 therapy [91]
	Entacapone	Compete with the catalytic site of FTO	HCC: Interfere with gluconeogenesis through FOXO1 [92]
	FB23/FB23-2	Directly bind to FTO and inhibit demethylase activity	AML: Suppress proliferation and promote differentiation/apoptosis [93].
	FTO-04	Block the catalytic activity of FTO	GBM: Prevents neurosphere formation and self-Renewal [94].
	N-CDPCB	Competitive bind to a novel site of FTO and inhibit demethylase activity [95]	−
	MA/MA2	Inhibition of the catalytic activity of FTO	GBM: Inhibit GSC cell growth and self-renewal [88]
	MO-I-500	Inhibition of the catalytic activity of FTO	BC: Inhibit cell survival via decreasing FTO and IRX3 proteins [96]
	R-2HG	Suppress FTO activity	AML, GBM: Inhibit proliferation/survival of FTO-high cancer cells [97]
	Rhein	Competitive bind to FTO catalytic domain	AML: Prevent or override tyrosine kinase inhibitor resistance [98] BC: Decrease tumor growth [99]
	Saikosaponin-d	Occupy the substrate-binding site of FTO	AML: suppress cell proliferation, promote apoptosis/cell-cycle arrest [100]