Table 2 Small molecules facilitating somatic cell reprogramming and their function

From: Generation of pluripotent stem cells without the use of genetic material

Small molecules	C ^a	Host animal	Function	TFs to be replaced or function	Reference
5-aza-CR, AZA	0.5 mM	Mouse	DMNT inhibitor	Promotion of reprogrammming	⁷⁷
RG108	0.04–500 μM	Mouse	DMNT inhibitor	Sox2 (with BIX) or Oct4	⁶³
RSC133	10 μM	Human	DMNT inhibitor, Histone deacetylase inhibitor	Promotion of reprogramming	⁸²
Sodium butyrate	0.5–1 mM	Mouse, human	HDAC inhibitor	Promotion of reprogramming	⁷⁹
SAHA	5 μM	Mouse	HDAC inhibitor	Promotion of reprogramming	⁴²
TSA	20 nM	Mouse	HDAC inhibitor	Promotion of reprogramming	⁴²
VPA	0.5–2 mM	Mouse, human	HDAC inhibitor	Promotion of reprogramming	¹⁵
Tranylcypromine (Parnate)	5–10 μM	Mouse	H3K4 demethylation inhibitor (epigenetic modulator)	Promotion of reprogramming	⁷¹
BIX	0.5–2 μM	Mouse	G9a HMTase inhibitor	Oct4	⁶⁷
CHIR	3–10 μM	Mouse, human	GSK-3β inhibitor that activate Wnt signalling pathway	Sox2	¹⁵
Kenpaullone	5 μM	Mouse	GSK-3/CDKs inhibitor	Klf4	⁷⁵
Compound B6	1 μM	Mouse	AKt-mediated inhibitor of GSK3-β	Promotion of reprogramming	⁸⁴
LiCl	5–10 mM	Mouse and human	GSK-3β inhibitor, LSD1 inhibitor	Promotion of reprogramming	⁷⁰
616452 (E-616452, RepSox)	1 μM	Mouse, human	TGF-β inhibitor (ALKinhibitor II)	Sox2	⁶⁹
A83-01	0.5 μM	Mouse, human	TGF-β inhibitor	Promotion of reprogramming	⁴³
LY-364947	1 μM	Mouse	TGF-β inhibitor	Sox2	⁷²
SB431542	2 μM	Mouse, human	TGF-β inhibitor	Promotion of reprogramming	⁷¹
PD0325901 (PD)	0.5–1 μM	Mouse, human	MEK inhibitor	Promotion of reprogramming	⁶⁷
AMI-5	5 μM	Mouse	Protein arginine methyltransferase inhibitor	Sox2, Klf4 (with A-83-01)	⁷³
N-oxaloylglycine	1 μM	Human	Prolyl-4-hydroxylase inhibitor	Promotion of reprogramming	⁴³
Compound B4 (TGFb-RI )	1 μM	Mouse	ALK4 inhibitor	Promotion of reprogramming	⁸⁴
Dasatinib	0.5 μM	Mouse	Src family tyrosine kinase inhibitor	Sox2	⁷²
iPY razine (iPY)	10 μM	Mouse	Src family tyrosine kinase inhibitor	Sox2	⁷²
PP1	10 μM	Mouse	Src family tyrosine kinase inhibitor	Sox2	⁷²
Rapamycin	0.3 nM	Mouse	mTOR inhibitor	Promotion of reprogramming	⁸³
Compound B8	1–2 μM	Mouse	IP3K inhibitor	Promotion of reprogramming	⁸⁴
Compound B10	1–2 μM	Mouse	P38 kinase inhibitor	Promotion of reprogramming	⁸⁴
D4476	5 μM	Mouse	CK1 inhibitor	Oct 4 with FSK and 2-Me-5HT	¹⁷
BayK	2 μM	Mouse	a L-channel calcium agonist	Sox2	⁶³
FSK	10–50 μM	Mouse	cAMP agonist	Oct4 with 2-Me-5HT), and D4476	¹⁷
Prostaglandin E2	5 μM	Mouse	cAMP agonist	Promotion of reprogramming	¹⁷
Rolipram	10 μM	Mouse	cAMP agonist	Promotion of reprogramming	¹⁷
2-Me-5HT	5 μM	Mouse	5-HT3 agonist	Oct4 with FSK and D4476	¹⁷
5-(4-Chloro-phenyl)-3-phenyl-pent-2-enoic acid (PS48)	5 μM	human	PDK1 activator	Promotion of reprogramming	⁴³
8-Br-cAMP	0.1–0.5 mM	Human	cAMP-dependent protein kinase activator	Promotion of reprogramming	⁶⁵
Fructose 2,6-bisphosphate	10 mM	Human	Phosphofructokinase 1 activator	Promotion of reprogramming	⁴³
Quercetin	1 μm	Human	Hypoxia-inducible factor pathway activator	Promotion of reprogramming	⁴³
DZNep	0.05–0.1 μM	Mouse	Epigenetic modulators	Promotion of reprogramming	¹⁷
DNP	1 μM	Human	Oxidative phosphorylation uncoupler	Promotion of reprogramming	⁴³
TTNPB	1 μM	Mouse	Retinoic acid receptor ligand	Promotion of reprogramming	¹⁷
Oxysterol	0.5–1 μM	Mouse	Sonic hedgehog signaling	Sox2, Klf4, and C-Myc	⁷⁴
Purmorphamine	0.5–1 μM	Mouse	Sonic hedgehog signaling	Sox2, Klf4, and C-Myc	⁷⁴
Shh	500 ng/ml	Mouse	Sonic hedgehog signaling	Sox2, Klf4, and C-Myc	⁷⁴

Abbreviations: BayK, Bay K8644; BIX, BIX-01294; CHIR, CHIR99021; CK1, Casein kinase 1; DNMT, DNA methyltransferase; DNP, 2,4-dinitrophenol; DZNep, 3-deazaneplanocin; FSK, forkolin; HDAC, histon deacetylase; G9a HMTase, G9a histone methyltransferase; IP3K, inositol triphosphate 3-kinase; PDK1, 3′-phosphoinositide-dependent kinase 1; SAHA, suberoylanilide hydroxamic acid; TF, transcription factor; TSA, trichostain A; VPA, valproic acid; 2-Me-5HT, 2-methyl-5-hydroxytryptamine; 5-aza-CR, AZA, 5-azacytidine; 8-Br-cAMP, 8-Bromoadenosine 3′′5′′-cyclic monophosphate.
^aC; Concentration used typical reprogramming experiments.

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Table 2 Small molecules facilitating somatic cell reprogramming and their function

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