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Cat. No.: HY-181955

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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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화학식: C₃₀H₂₄N₄O₃
분자량:488.54

보관:

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

MS1129 Chemical Structure

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

DNMT1

DNMT3A

DNMT3B

Caspase-10

Caspase-3

Caspase-7

All DNA Methyltransferase Isoforms :

All HIF/HIF Prolyl-Hydroxylase Isoforms :

All Caspase Isoforms :

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.

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	T_1/2	T_max	C_max	AUC_last	V_z/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.

Chemical Information

분자량 488.54
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. Wang Y, et al. HIF-activated priming of TRAIL-induced cell death determines epigenetic vulnerability in kidney cancer. Cell Rep Med. 2026;7(3):102630. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

MS1129

All DNA Methyltransferase Isoforms

All HIF/HIF Prolyl-Hydroxylase Isoforms

All Caspase Isoforms