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. 2013 Apr 22;34(6):765–776. doi: 10.1038/aps.2013.21

Table 2. Summary of small molecule compounds enhancing iPSC generation.

Name Targets Effects Ref
Chemicals protomoting reprogramming
Epigenetic modifiers
Valproic acid HDAC inhibitor Promote KOS-induced reprogramming, enable the reprogramming of human fibroblasts transduced by OS 56,57
TSA HDAC inhibitor Promote OSKM-induced reprogramming 56
SAHA HDAC inhibitor Promote OSKM-induced reprogramming 56
RG108 DNMT inhibitor In combination with BIX to improve KO-induced MEF reprogramming 58
5-AZA DNMT inhibitor Promote OSKM-induced reprogramming 56
BIX-01294 HMTase G9a inhibitor Promote reprogramming of NPCs and MEFs transduced by OK 58,102
Parnate LSD1 inhibitor Enable the reprogramming of human keratinocytes transduced by OK 59
LiCl Inhibitor of LSD1 and GSK3 Promote MEF reprogramming by OSKM 60
Vitamin C Vitamin-C-dependent H3K36 demethylase (Jhdm1a/1b), antioxident, p53, senescence Enhance iPSC generation from both mouse and human somatic cells 91
Anisomycin and TNF-α Activation of p38, reducing the global DNA methylation Promote MEF reprogramming by OSKM 62
EMT/MET modulators
SB-431542 ALK4/5/7 inhibitor Replace c-myc or Sox2 to promote MEF reprogramming 69
E-616452 (RepSox) ALK5 inhibitor Promote reprogramming, replace Sox2 in reprogramming 70
A-83-01 ALK5 inhibitor Combined with MEK and Rock inhibitors to improve human fibroblast reprogramming; support rat iPSC long-term selfrenewal when combined with CHIR99021 and PD0325901 68,103
Thiazovivin ROCK inhibitor Increase reprogramming efficiency and accelerate reprogramming kinetics of human fibroblasts in conjunction with MEK and TGF inhibitors 103
Metabolic regulator (glycolysis pathway)
PS48 Activator of PDK1/PI3K/Akt Promote human iPSC induction by Oct4 alone 75
Fructose 6-phosphate Stimulate glycolytic metabolism Promote human iPSC induction by Oct4 alone 75
Fructose 2,6-bisphosphate Stimulate glycolytic metabolism Promote human iPSC induction by Oct4 alone 75
Nicotinic acid Stimulate glycolytic metabolism Promote human iPSC induction by Oct4 alone 75
2-Hydroxyglutaric acid (2-HA) Stimulate glycolytic metabolism Promote human iPSC induction by Oct4 alone 75
Quercetin HIF pathway activation Promote human iPSC induction by Oct4 alone 75
N-oxaloylglycine (NOG) HIF pathway activation Promote human iPSC induction by Oct4 alone 75
2,4-dinitrophenol (DNP) Uncouple the mitochondrial respiratory chain Promote human iPSC induction by Oct4 alone 75
Other chemicals promoting reprogramming
(+)Bayk 8644 L-type Ca2+ channel Promote MEF reprogramming in combination with G9a inhibition 58
CD437 RAR agonist Promote OSKM-induced reprogramming 92
AM580 RAR agonist Promote OSKM-induced reprogramming 92
Dexamethasone Steroid glucocorticoid Promote OSKM-induced reprogramming 56
Rapamycin Inhibitor of mTOR Promote OSKM-induced reprogramming 94
PP242 Inhibitor of mTOR Promote OSKM-induced reprogramming 94
Resveratrol Sirtuin activator Promote OSKM-induced reprogramming 94
Fisetin Sirtuin activator Promote OSKM-induced reprogramming 94
Spermidine An autophagy inducer Promote OSKM-induced reprogramming 94
LY294002 PI3K inhibitor Promote OSKM-induced reprogramming 94
Curcumin An antioxidant Promote OSKM-induced reprogramming 94
Chemicals facilitating self-renewal of stem cells
PD0325901+CHIR99021 (2i) Inhibitor of MEK and GK3 respectively Eliminate differentiation of stem cells 87
6-Bromoindirubin-3′-oxime (BIO) GSK-3 inhibitor IX Maintain human and mouse ESCs in an undifferentiated state without feeder cells 88
Pluripotin/SC1 RasGAP and ERK1 Support mESC self-renewal 86
Y-27632 ROCK inhibitor Enhance survival rate after cryopreservation and cloning efficiency of human ES and iPSCs 104

iPSC, induced pluripotent stem cell; K, Klf4; O, Oct4; M, c-Myc; S, Sox2