2. PROTAC Epigenetics
  3. Molecular Glues DNA Methyltransferase
  4. DNMT1 Degrader-1

DNMT1 Degrader-1 是一种选择性 DNMT1 降解剂，IC50 为 202.87 nM，Kd 值为 122 nM。DNMT1 Degrader-1 可作为分子胶与 DNMT1 和 UHRF1 形成三元复合物，触发 UHRF1 介导的 DNMT1 泛素化与降解，并抑制 DNMT1 的酶活性。DNMT1 Degrader-1 可抑制原代急性髓系白血病细胞的增殖，发挥抗肿瘤活性。DNMT1 Degrader-1 可用于急性髓系白血病的研究。

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DNMT1 Degrader-1

DNMT1 Degrader-1 Chemical Structure

CAS No. : 2962943-72-0

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DNMT1 Degrader-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DNMT1 Degrader-1 is a selective DNMT1 degrader with an IC50 of 202.87 nM and a Kd value of 122 nM. As a molecular glue, DNMT1 Degrader-1 forms a ternary complex with DNMT1 and UHRF1, thereby triggering UHRF1-mediated ubiquitination and degradation of DNMT1, and inhibiting the enzymatic activity of DNMT1. DNMT1 Degrader-1 inhibits the proliferation of primary acute myeloid leukemia cells and exerts anti-tumor activity. DNMT1 Degrader-1 can be used for the research of acute myeloid leukemia[1].

IC50 & Target[1]

DNMT1

 

体外研究
(In Vitro)

DNMT1 Degrader-1 (compound 6k) (0-2000 nM; 0-24 h) 可在 MV-4-11 急性髓系白血病 (AML) 细胞中诱导 DNMT1 蛋白呈时间和浓度依赖性降解，其 DC50 为 123.4 nM[1]。
DNMT1 Degrader-1 (0.25-1 μM; 24 h) 不会影响 Kasumi-1 或 MV-4-11 AML 细胞中的 DNMT1 mRNA 水平[1]。
DNMT1 Degrader-1(1 μM; 6 h) 可在 MV-4-11 急性髓系白血病 (AML) 细胞中诱导 DNMT1 蛋白发生泛素化，进而导致其蛋白酶体降解[1]。
DNMT1 Degrader-1 (1 μM; 0-24 h) 诱导 MV-4-11 急性髓系白血病 (AML) 细胞中 DNMT1 发生泛素化和降解的作用依赖于 UHRF1[1]。
DNMT1 Degrader-1 (72 h) 可抑制多种 AML 及血液癌细胞系的增殖[1]。
DNMT1 Degrader-1 (0.2-2 μM; 24 h) 可在 MV-4-11 和 Kasumi-1 急性髓系白血病 (AML) 细胞中诱导剂量依赖性细胞周期阻滞[1]。

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

DNMT1 Degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: MV-4-11 AML cells
Concentration: 0, 50, 100, 200, 400, 600, 800, 1000, 1500, 2000 nM
Incubation Time: 0, 6, 9, 12, 15, 24 h
Result: Induced time-dependent degradation of DNMT1 protein, with complete elimination observed by 24 h at 1 μM.
Induced concentration-dependent DNMT1 degradation with a DC50 of 123.4 nM after 24 h treatment.

Cell Cycle Analysis[1]

Cell Line: MV-4-11 and Kasumi-1 AML cells
Concentration: 0.2, 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Induced dose-dependent G1 phase accumulation with reduced cell numbers in S and G2/M phases in MV-4-11 cells.
Induced dose-dependent S phase accumulation with reduced cell numbers in G1 and G2/M phases in Kasumi-1 cells.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t AUC0-∞ T1/2 Tmax Cmax Bioavailability
Rat[1] 25 mg/kg p.o. 689 ng·h/mL 948 ng·h/mL 9.9 μg·h/mL 2.2 h 59.8 ng/mL 61 %
Rat[10] 10 mg/kg i.v. 546 ng·h/mL 613 ng·h/mL 6.6 h / / /
体内研究
(In Vivo)

DNMT1 Degrader-1 (40 mg/kg；腹腔注射；每日一次；连续 16 天) 在 MV‑4‑11 细胞衍生异种移植、WEHI‑3 原位移植及 AML 患者来源异种移植小鼠模型中显著抑制急性髓系白血病生长并延长生存期[1]。
DNMT1 Degrader-1 (40 mg/kg；腹腔注射；每日给药；连续 14 天) 在健康 BALB/c 小鼠中经 14 天每日腹腔注射给药后，表现出极低的体内血液学毒性[1]。

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

Animal Model: BALB/c mice (18-22 g, 6-8 weeks) with MV‑4‑11 subcutaneous xenografts or WEHI‑3 orthotopic transplantation; NOG mice (16-20 g, 6 weeks) with AML patient‑derived xenografts[1]
Dosage: 40 mg/kg
Administration: i.p.; daily; 16 days
Result: Markedly inhibited tumor growth in MV‑4‑11 xenograft mice, alleviated leukemia‑induced splenomegaly, reduced leukemic cell infiltration in liver and spleen.
Significantly prolonged the overall survival of WEHI‑3 orthotopic transplantation mice.
Obviously increased the survival rate of AML PDX mice, reduced the population of human CD45+ AML cells in bone marrow and peripheral blood, and showed potent in vivo anti‑AML efficacy with favorable safety.
分子量

408.54

Formula

C24H32N4O2
CAS 号
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

DNMT1 Degrader-1 相关分类

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Keywords:

DNMT1 Degrader-12962943-72-0Molecular GluesDNA MethyltransferaseDNMTsDNA MTasesG9aUHRF1DNMT3BDNMT3Aacute myeloid leukemiaKasumi-1 AML cellsMV-4-11 AML cellsDNMT1proteasome pathwaypatient-derived xenograft modelsInhibitorinhibitorinhibit

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