pdk-1 — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T2348	GSK2334470		PDK
	GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.		PDK
T1837	BX-912		Apoptosis , VEGFR , PKA , Chk , CDK , PDK
	BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc.		Apoptosis , VEGFR , PKA , Chk , CDK , PDK
T1830	BX795		IκB/IKK , Chk , CDK , c-Kit , PDK , Autophagy
	BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than...		IκB/IKK , Chk , CDK , c-Kit , PDK , Autophagy
T24677	PS47	PS 47,PS-47	PDK
	PS-47(PS 47) is an inactive E-isomer of PS48. PS48 is an activator of PDK1.		PDK
T12398	MP7	PDK1 inhibitor	PDK
	MP7 (PDK1 inhibitor) is a inhibitor of phosphoinositide-dependent kinase-1 (PDK1).		PDK
T4046	BX517	PDK1 inhibitor 2,BX 517,BX-517	Akt , PDK
	BX517 (PDK1 inhibitor 2) is a potent and selective inhibitor of PDK1.		Akt , PDK
T16670	PS210		PDK
	PS210 is a potent and selective activator of PDK1 (Kd: 3 μM), specifically targeting the PIF-binding pocket of PDK1, without acting against other protein kinases such as S6K, PKB/Akt, or GSK3. Its prodrug, PS423, serves ...		PDK
T74830	PDK-IN-1
	PDK-IN-1 (compound 7o), a pyruvate dehydrogenase kinase (PDK) inhibitor, exhibits IC50 values of 0.03 and 0.1 μM against PDK1 and HSP90, respectively. This compound effectively targets the PDH/PDK axis, significantly red...
T12412L	PDK4-IN-1 hydrochloride		Apoptosis , PDK
	PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4)(IC50 value of 84 nM)		Apoptosis , PDK
T3895	Polyphyllin I		Apoptosis , Akt , JNK , PDK , mTOR , Autophagy
	Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D ha...		Apoptosis , Akt , JNK , PDK , mTOR , Autophagy
T12412	PDK4-IN-1		Others
	PDK4-IN-1 is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4)(IC50 value of 84 nM).		Others
T16450	PDK1-IN-RS2		PDK
	PDK1-IN-RS2 inhibits the activation of the downstream kinases S6K1 by PDK1. PDK1-IN-RS2 is a mimic of the peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor (Kd: 9 μM).		PDK
T17224	VER-246608		Dehydrogenase , PDK
	VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively).VER-246608 disrupts Warburg metabolism an...		Dehydrogenase , PDK
T79723	PDK-IN-2
	PDK-IN-2 (Compound 1F), with an IC50 of 68 nM, is a potent PDK inhibitor that downregulates the expression of PDK1 and PDK4 in cells. It promotes mitochondrial bioenergetics, reduces glycolytic activity, and triggers apo...