2. Apoptosis Epigenetics Metabolic Enzyme/Protease
  3. Apoptosis DNA Methyltransferase HIF/HIF Prolyl-Hydroxylase Caspase
  4. MS1129

MS1129 is a DNMT degrader that induces proteasomal degradation of DNMT1, DNMT3A and DNMT3B proteins. MS1129 upregulates TRAIL, DR4 and DR5 proteins, downregulates the decoy receptor DcR2, and activates TRAIL-dependent apoptosis via the HIF-1/2 and Caspase-10 pathways. MS1129 is applicable to the research of VHL-deficient clear cell renal cell carcinoma.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

MS1129

MS1129 Chemische Struktur

Größe Verfügbarkeit
50 mg   Angebot einholen  
100 mg   Angebot einholen  
250 mg   Angebot einholen  

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

This product is a controlled substance and not for sale in your territory.

MS1129 Related Antibodies

Top Publications Citing Use of Products

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
DNA Methyltransferase DNMT1 DNMT3 MGMT

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
HIF-1α HIF

Alle Caspase Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • Biologische Aktivität

  • Reinheit & Dokumentation

  • Verweise

  • Kundenbewertung

Beschreibung

MS1129 is a DNMT degrader that induces proteasomal degradation of DNMT1, DNMT3A and DNMT3B proteins. MS1129 upregulates TRAIL, DR4 and DR5 proteins, downregulates the decoy receptor DcR2, and activates TRAIL-dependent apoptosis via the HIF-1/2 and Caspase-10 pathways. MS1129 is applicable to the research of VHL-deficient clear cell renal cell carcinoma[1].

IC50 & Target[1]

DNMT1

 

DNMT3A

 

DNMT3B

 

Caspase-10

 

Caspase-3

 

Caspase-7

 

In Vitro

MS1129 (2 μM; 3 days) induces robust apoptosis in parental VHL-deficient RCC10 clear cell renal cell carcinoma cells, and this effect is dependent on the expression of HIF-1α/2α[1].
MS1129 inhibits the viability of parental VHL-deficient RCC10 clear cell renal cell carcinoma (ccRCC) cells with an IC50 of 1.3 μM, while its potency decreases in HIF-1α/2α double knockout (DKO) RCC10 cells (IC50 = 3.2 μM)[1].
MS1129 (2 μM; 0-48 h) induces time-dependent proteasomal degradation of DNMT1, DNMT3A and DNMT3B proteins in RCC10 clear cell renal cell carcinoma cells, with the maximum degradation level reached at 48 h[1].
MS1129 (1-3 μM; 2 days) induces apoptosis in RCC10 clear cell renal cell carcinoma (ccRCC) cells by activating caspase-3, caspase-7 and PARP1, while the pan-caspase inhibitor Z-VAD-FMK (HY-16658B) partially inhibits this effect[1].
MS1129 (2 μM; 2 days) activates the TRAIL death receptor signaling pathway in RCC10 ccRCC cells by upregulating TRAIL, DR4 and DR5, downregulating DcR2, and inducing caspase-10 cleavage[1].

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

MS1129 Related Antibodies

Apoptosis Analysis[1]

Cell Line: Parental VHL-deficient RCC10 ccRCC cells, HIF-1α/2α-DKO RCC10 ccRCC cells
Concentration: 2 μM
Incubation Time: 3 days
Result: Induced robust cell death in parental RCC10 cells, resulting in ~80% PI-positive cells.
Showed minimal PI-positive cells in HIF-1α/2α-DKO RCC10 cells, comparable to vehicle controls.

Western Blot Analysis[1]

Cell Line: RCC10 ccRCC cells
Concentration: 2 μM (MS1129); 10 μM MG132 (co-treatment); 2 μM MG262 (co-treatment)
Incubation Time: 0, 12, 18, 24, 36, 48 h (MS1129); 6 h (MG132 after 36 h MS1129); 2 h (MG262 after 36 h MS1129)
Result: Induced time-dependent proteasomal degradation of DNMT1, DNMT3A, and DNMT3B proteins, with degradation detectable as early as 12 h and progressing through 48 h.
Blocked degradation of DNMT proteins when co-treated with proteasome inhibitors MG132 or MG262.

Apoptosis Analysis[1]

Cell Line: RCC10 ccRCC cells
Concentration: 1-3 μM (MS1129); 2 μM (MS1129 with Z-VAD-FMK); 20 μM Z-VAD-FMK (pre-treatment)
Incubation Time: 2 days (1-3 μM MS1129); 3 days (2 μM MS1129 with Z-VAD-FMK); 30 min (Z-VAD-FMK pre-treatment)
Result: Induced dose-dependent increases in cleaved caspase-3, cleaved caspase-7, and cleaved PARP1 levels in RCC10 cells after 2 days of treatment.
Reduced PI-positive cells from ~80% to ~30% when cells were pre-treated with 20 μM Z-VAD-FMK prior to 2 μM MS1129 treatment for 3 days.

Western Blot Analysis[1]

Cell Line: RCC10 ccRCC cells
Concentration: 2 μM
Incubation Time: 2 days
Result: Upregulated protein levels of TRAIL, DR4, and DR5.
Downregulated protein levels of decoy receptor DcR2.
Induced cleavage of procaspase-10 to active cleaved caspase-10.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUClast Vz/F CL/F MRT
Mice[1] 5 mg/kg i.p. 294 min 90 min 618 ng/mL 178978 min·ng/mL 11359 mL 26.8 mL/min 352 min
In Vivo

MS1129 (5 mg/kg; i.p.; daily; 10 days) significantly inhibits the growth of subcutaneous 786-O ccRCC xenografts in NSG mice without altering body weight[1].

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

Animal Model: NSG (NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ) (male, 6-8 weeks old, subcutaneous implantation of 786-O cells)[1]
Dosage: 5 mg/kg
Administration: i.p.; daily; 10 days
Result: Reduced tumor volume relative to vehicle controls.
Lowered tumor weights significantly compared to vehicle-treated mice.
Remained stable in mouse body weight throughout treatment.
Molekulargewicht

488.54

Formel

C30H24N4O3
SMILES

COC1=C(C=CC=C1)C(NC2=CC=C(C=C2)NC(C3=CC=C(C=C3)NC4=CC=NC5=C4C=CC=C5)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

MS1129 Related Classifications

  • Molaritätsrechner

  • Verdünnungsrechner

Die Formel zur Berechnung von Molaritäten

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)

Diese Gleichung wird häufig abgekürzt als: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

MS1129MS 1129MS-1129ApoptosisDNA MethyltransferaseHIF/HIF Prolyl-HydroxylaseCaspaseDNMTsDNA MTasesHypoxia-inducible factorsHIFsHIF-PHNSG miceTNFRSF10ADNMT3BVHL-deficient ccRCC cellsDNMT1patient-derived xenografts786-O ccRCC cellsDNMT3ATNFRSF10BTNFSF10Inhibitorinhibitorinhibit

Ihre kürzlich angesehenen Produkte:

Online-Anfrage

Your information is safe with us. * Required Fields.

Produktname

  

Requested Quantity *

Name des Antragstellers *

 

Anrede

E-Mail-Addresse *

 

Telefonnummer *

Department

 

Name der Organisation *

City

Bundesland

Country or Region *

      

Bemerkungen

Massenanfrage

Inquiry Information

Produktname:
MS1129
Art. -Nr.:
HY-181955
Menge:
MCE Japan Authorized Agent:

Kundenbewertung

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Produktname

  

Lot #

Name des Antragstellers *

 

E-Mail-Addresse *

Telefonnummer

 

Department *

Name der Organisation *

 

Country or Region *

Bemerkungen

SAFETY DATA SHEET (SDS)

Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.