1. Epigenetics TGF-beta/Smad Cell Cycle/DNA Damage
  2. PKC Histone Methyltransferase DNA Methyltransferase DNA/RNA Synthesis
  3. Go 6983

Go 6983 GMP is Go 6983 (HY-13689) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Go 6983 is a dual inhibitor targeting Suv39h1/2 (KMT1A/KMT1B) and PKC, as well as a transcriptional activator capable of inducing DNA hypomethylation. Go 6983 stimulates the transcription of Prdm14 by reducing Suv39h1/2 protein levels, decreasing histone modifications in the Prdm14 promoter region, and increasing the recruitment of RNA polymerase II. Go 6983 induces genome-wide DNA hypomethylation by inhibiting de novo methyltransferase expression and increasing Tet1/Tet2 levels, thereby promoting self-renewal and pluripotency maintenance of stem cells. Meanwhile, Go 6983 can block PKC-mediated signaling pathways to reduce the expression of EMT-related genes and eliminate the upregulation of antioxidant genes downstream of NRF2. Go 6983 is mainly used in mechanism studies related to myocardial ischemia/reperfusion injury.

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Go 6983

Go 6983 Chemical Structure

CAS No. : 133053-19-7

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Description

Go 6983 GMP is Go 6983 (HY-13689) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Go 6983 is a dual inhibitor targeting Suv39h1/2 (KMT1A/KMT1B) and PKC, as well as a transcriptional activator capable of inducing DNA hypomethylation. Go 6983 stimulates the transcription of Prdm14 by reducing Suv39h1/2 protein levels, decreasing histone modifications in the Prdm14 promoter region, and increasing the recruitment of RNA polymerase II. Go 6983 induces genome-wide DNA hypomethylation by inhibiting de novo methyltransferase expression and increasing Tet1/Tet2 levels, thereby promoting self-renewal and pluripotency maintenance of stem cells. Meanwhile, Go 6983 can block PKC-mediated signaling pathways to reduce the expression of EMT-related genes and eliminate the upregulation of antioxidant genes downstream of NRF2. Go 6983 is mainly used in mechanism studies related to myocardial ischemia/reperfusion injury[1][2][3].

IC50 & Target

DNMT3A

 

SUV39H2/KMT1B

 

In Vitro

Go 6983 GMP (5 μM; 8 d) promotes short-term self-renewal and maintains pluripotency of 46C mouse embryonic stem cells in both serum-containing medium without LIF and serum-free N2B27 medium[1].
Go 6983 GMP (5 μM; 8 d) promotes the self-renewal of 46C mouse embryonic stem cells via Prdm14, as overexpression of Prdm14 mimics the activity of Go6983, while knockdown of Prdm14 abolishes Go6983-mediated pluripotency maintenance[1].
Go 6983 GMP (5 μM; 24 h) promotes short-term self-renewal of human induced pluripotent stem cells, and this effect is mediated by Prdm14 through inhibiting the expression of Dnmt3 gene[1].
Go 6983 GMP (5 μM; 12 h, 24 h) enhances the expression of Prdm14 in 46C mouse embryonic stem cells by reducing the expression levels of Suv39h1 and Suv39h2[1].
Go 6983 (5 μM) blocks Dihydrotanshinone I (HY-N0360)-induced NRF2 nuclear accumulation by inhibiting nuclear import, and this process cannot be reversed by the nuclear export inhibitory effect of leptomycin B in HL-1 mouse cardiomyocytes[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Prdm14 expression in 46C mouse embryonic stem cells
Concentration: 5 μM
Incubation Time: 12 h, 24 h
Result: Enhanced Prdm14 expression by reducing Suv39h1 and Suv39h2 levels, which alleviated repressive H3K9me2 and H3K9me3 marks at the Prdm14 promoter and increased RNA polymerase II recruitment and elongation.
Molecular Weight

442.51

Formula

C26H26N4O3

CAS No.
SMILES

O=C(C(C1=CN(CCCN(C)C)C2=C1C=C(OC)C=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Go 6983
Cat. No.:
HY-13689G
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