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

MS1129 是一种 DNMT 降解剂，可诱导 DNMT1、DNMT3A 和 DNMT3B 蛋白的蛋白酶体降解。MS1129 可上调 TRAIL、DR4 和 DR5 蛋白，下调诱饵受体 DcR2，并通过 HIF-1/2 和 Caspase-10 通路激活 TRAIL 依赖性凋亡 (apoptosis)。MS1129 可用于 VHL 缺陷型透明细胞肾细胞癌的研究。

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MS1129

MS1129 Chemical Structure

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MS1129 相关抗体

Top Publications Citing Use of Products

查看 DNA Methyltransferase 亚型特异性产品:

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DNA Methyltransferase DNMT1 DNMT3 MGMT

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HIF-1α HIF

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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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

MS1129 (2 μM; 3 days) 可在亲本 VHL 缺陷型 RCC10 肾透明细胞癌细胞中诱导强烈的细胞凋亡，该效应依赖于 HIF-1α/2α 的表达[1]。
MS1129 可抑制亲本 VHL 缺陷型 RCC10 肾透明细胞癌 (ccRCC) 细胞的活力，其 IC50 为 1.3 μM；而在 HIF-1α/2α 双敲除 (DKO) RCC10 细胞中，其效力降低 (IC50 = 3.2 μM)[1]。
MS1129 (2 μM; 0-48 h) 可在 RCC10 肾透明细胞癌细胞中诱导 DNMT1、DNMT3A 和 DNMT3B 蛋白发生时间依赖性蛋白酶体降解，在 48 h 时降解程度达到峰值[1]。
MS1129 (1-3 μM; 2 days) 可通过激活 caspase-3、caspase-7 和 PARP1 诱导 RCC10 肾透明细胞癌 (ccRCC) 细胞发生凋亡，而泛半胱天冬酶抑制剂 Z-VAD-FMK (HY-16658B) 可部分抑制该作用[1]。
MS1129 (2 μM; 2 days) 可通过上调 TRAIL、DR4 和 DR5、下调 DcR2 并诱导 caspase-10 切割，在 RCC10 ccRCC 细胞中激活 TRAIL 死亡受体信号通路[1]。

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

MS1129 相关抗体:

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.
药代动力学
(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
体内研究
(In Vivo)

MS1129 (5 mg/kg；腹腔注射；每日一次；连续 10 天) 可显著抑制 NSG 小鼠皮下 786-O 肾透明细胞癌 (ccRCC) 异种移植物的生长[1]。

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.
分子量

488.54

Formula

C30H24N4O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MS1129 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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