DS-437
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- CAS-Nr.
- 1674364-87-4
- Englisch Name:
- DS-437
- Synonyma:
- DS-437;DS-437
(DS437;DS-437 >=98% (HPLC);Adenosine, 5'-S-[2-[[(ethylamino)carbonyl]amino]ethyl]-5'-thio-
- CBNumber:
- CB74669958
- Summenformel:
- C15H23N7O4S
- Molgewicht:
- 397.45
- MOL-Datei:
- 1674364-87-4.mol
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DS-437 Eigenschaften
- Dichte
- 1.71±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- L?slichkeit
- DMSO:125.0(Max Conc. mg/mL);314.5(Max Conc. mM)
- pka
- 13.13±0.70(Predicted)
- Aggregatzustand
- powder
- Farbe
- white to beige
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
RIDADR |
UN 2811 6.1 / PGIII |
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Bildanzeige (GHS) |
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Alarmwort |
Achtung |
Gefahrenhinweise |
Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
H301 |
Giftig bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 3 |
Achtung |
src="/GHS06.jpg" width="20" height="20" /> |
P264, P270, P301+P310, P321, P330,P405, P501 |
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Sicherheit |
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DS-437 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
DS-437 is a dual inhibitor of protein arginine methyltransferase 5 (PRMT5) and PRMT7 (IC
50s = 5.9 and 6 μM, respectively). It is selective for PRMT5 and PRMT7 over a panel of 29 additional protein, DNA, and RNA methyltransferases at 50 μM, but also inhibits DNMT3A and DNMT3B (IC
50s = 52 and 62 μM, respectively). DS-437 (2.5 and 10 μM) inhibits symmetrical arginine dimethylation of FOXP3 in HEK293T cells, as well as symmetrical arginine dimethylation of p60 and the ribonucleoproteins SmD1/D3 and SmB/B’ in MDA-MB-231 cells in a concentration-dependent manner. It inhibits the ability of regulatory T cells (Tregs) to suppress effector T cell (Teff) proliferation
in vitro in human and murine Treg suppression assays. DS-437 (10 mg/kg five times per week) reduces tumor growth in a CT26Her2 murine colon cancer model when administered in combination with the anti-p185
erbB2/neu antibody 4D5.
Verwenden
DS-437 has been used as an inhibitor of protein arginine methyltransferase 5 (PRMT5) to study its effect on forkhead box P3 (FOXP3) methylation and regulatory T cells (Tregs) function in 293T cells.
Biochem/physiol Actions
DS-437 is an analog of S-adenosyl methionine (SAM ), which inhibits protein arginine methyltransferases PRMT5 and PRMT7 (IC50 5.9 and 6 μM) with little interaction against a panel of 30 other human methyltransferases.
DS-437 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
DS-437 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 17)Lieferanten
- DS-437
- DS-437
(DS437
- Adenosine, 5'-S-[2-[[(ethylamino)carbonyl]amino]ethyl]-5'-thio-
- DS-437 >=98% (HPLC)
- 1674364-87-4
- C15H23N7O4S