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.

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MS1129

MS1129 Chemical Structure

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MS1129 Related Antibodies

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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

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Description

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.
Molecular Weight

488.54

Formula

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MS1129 Related Classifications

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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

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