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