2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. PROTAC PRMT1 degrader-1

PROTAC PRMT1 degrader-1 (compound 4) 是一种 PRMT1 PROTAC 降解剂，对人源 PRMT1 的 IC50 为 185.7 nM。PROTAC PRMT1 degrader-1 可招募 CRBN E3 泛素连接酶，诱导 PRMT1 发生蛋白酶体依赖性降解；它还能与 PRMT1 和 CRBN 形成三元复合物，促使 PRMT1 发生泛素化并随后被蛋白酶体降解。PROTAC PRMT1 degrader-1 可降低癌细胞中不对称二甲基精氨酸的水平，以及组蛋白 H4 上精氨酸 3 的不对称二甲基化水平，同时抑制多种癌细胞的生长。PROTAC PRMT1 degrader-1 可用于乳腺癌、黑色素瘤的研究。
(粉色: Histone Methyltransferase 配体 (HY-182297)；蓝色: Cereblon 配体 (HY-14658)；黑色: 连接子 (HY-133388))。

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PROTAC PRMT1 degrader-1

PROTAC PRMT1 degrader-1 Chemical Structure

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PROTAC PRMT1 degrader-1 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Histone Methyltransferase 亚型特异性产品:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with an IC50 of 185.7 nM against human PRMT1. PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma[1]. (Pink: Histone Methyltransferase ligand (HY-182297); Blue: Cereblon ligand (HY-14658); Black: linker (HY-133388)).

体外研究
(In Vitro)

PROTAC PRMT1 degrader-1 (compound 4) (1 μM) 在 AlphaLISA 生化分析中，以 1 μM 浓度处理时对纯化的 PRMT1 甲基转移酶活性的抑制率达 86.2%，IC50 为 185.7 nM；同时在相同分析体系中对其他 I 型 PRMT 酶也具有抑制活性[1]。
PROTAC PRMT1 degrader-1 (compound 4) (0.1-5 μM; 3-96 h) 可在人乳腺癌 MCF-7 细胞中诱导 PRMT1 呈浓度和时间依赖性降解，其 DC50 为 0.77 μM，Dmax 为 84.83%，且在处理后 6 h 即可检测到降解现象[1]。
PROTAC PRMT1 degrader-1 (compound 4) (0.1-5 μM; 48 h) 可在人黑色素瘤 A2058 细胞中诱导 PRMT1 的浓度依赖性降解，其 DC50 为 0.65 μM，Dmax 为 93.03%[1]。
PROTAC PRMT1 degrader-1 (compound 4) (0.1-5 μM; 48 h) 可在人癌细胞 MDA-MB-231、MDA-MB-468 和 A375 中诱导 PRMT1 的浓度依赖性降解，在 A375 细胞中的 DC50 为 0.52 μM，Dmax 为 88.36%[1]。
PROTAC PRMT1 degrader-1 (compound 4) (2 μM; 12-96 h) 可在人乳腺癌 MCF-7 细胞中选择性降解 PRMT1，而不降解 PRMT3、PRMT4、PRMT6 和 PRMT8，同时也不会降解常见的 CRBN 新底物 GSPT1、IKZF1 或 IKZF3[1]。
PROTAC PRMT1 degrader-1 (compound 4) (2 μM; 12-96 h) 可在人乳腺癌 MCF-7 细胞中以时间依赖的方式降低整体不对称二甲基精氨酸水平和组蛋白 H4R3me2a 水平[1]。
PROTAC PRMT1 degrader-1 (compound 4) (1.25-5 μM; 5 days) 对 MCF-7 人乳腺癌细胞和 A2058 人黑色素瘤细胞表现出持续 5 天的剂量依赖性生长抑制作用，其活性强于母本抑制剂 DCPT2145，且 A2058 细胞对其敏感性更高[1]。
PROTAC PRMT1 degrader-1 (compound 4) (0.63-10 μM; 14 days) 可在 2.5 μM 及以上浓度下抑制人乳腺癌细胞 MCF-7 的集落形成，在 1.25 μM 及以上浓度下抑制人黑色素瘤细胞 A2058 的集落形成，且 A2058 细胞表现出更高的敏感性[1]。
PROTAC PRMT1 degrader-1 (compound 4) (1 μM; 0-60 min) 在小鼠肝微粒体中具有中等代谢稳定性，半衰期为 26.0 min，固有清除率为 211 mL/min/kg[1]。

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

PROTAC PRMT1 degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 0.1-5 μM (48 h concentration-dependent); 5 μM (time-course); 2 μM (time-course)
Incubation Time: 3-96 h (time-course); 48 h (concentration-dependent)
Result: Reduced PRMT1 protein levels by 40%, 60%, and 86.5% respectively at 0.2, 1, 5 μM for 48 h.
Induced concentration-dependent PRMT1 degradation with a DC50 of 0.77 μM and a maximum degradation (Dₘₐₓ) of 84.83% at 0.1, 0.3, 0.5, 1, 3, 5 μM for 48 h.
Induced detectable PRMT1 degradation as early as 6 h, with near-maximal degradation observed at 48 h at 5 μM.
Caused significant PRMT1 degradation at 48 h, with maximum degradation achieved between 72-96 h at 2 μM.

Western Blot Analysis[1]

Cell Line: A2058 human melanoma cells
Concentration: 0.1-5 μM
Incubation Time: 48 h
Result: Induced concentration-dependent PRMT1 degradation with a DC50 of 0.65 μM and a Dₘₐₓ of 93.03%.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, MDA-MB-468, A375 human cancer cells
Concentration: 0.1-5 μM (A375 cells only)
Incubation Time: 48 h (A375 cells only)
Result: Reduced PRMT1 protein levels in a concentration-dependent manner in MDA-MB-231 and MDA-MB-468 cells.
Induced concentration-dependent PRMT1 degradation with a DC50 of 0.52 μM and a Dₘₐₓ of 88.36% in A375 cells.

Western Blot Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 2 μM
Incubation Time: 12-96 h
Result: Reduced PRMT1 protein levels in a time-dependent manner, but had no significant effect on PRMT3, PRMT4, or PRMT6 protein levels over 12-96 h, and only slightly reduced PRMT8 protein levels at 96 h.
Did not degrade CRBN neosubstrates GSPT1, IKZF1, or IKZF3 at these concentrations and time points.\nInduced a time-dependent reduction in global aDMA levels and asymmetric dimethylation of histone H4 arginine 3 (H4R3me2a) levels, consistent with PRMT1 degradation kinetics.

Cell Viability Assay[1]

Cell Line: MCF-7 human breast cancer cells, A2058 human melanoma cells
Concentration: 1.25-5 μM
Incubation Time: 5 days
Result: Showed stronger dose-dependent growth inhibition than the parental inhibitor DCPT2145 at all tested concentrations over 5 days in MCF-7 cells.
Showed stronger dose-dependent growth inhibition than DCPT2145 at all tested concentrations over 5 days in A2058 cells, with greater sensitivity observed in A2058 cells compared to MCF-7 cells.
分子量

752.94

Formula

C43H56N6O6
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

PROTAC PRMT1 degrader-1 相关分类

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  • 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:

PROTAC PRMT1 degrader-1PROTACsHistone MethyltransferaseCRBNmelanomaPRMT1breast cancerA2058 human melanoma cellshistone H4proteasomeMCF-7 human breast cancer cellsasymmetric dimethylarginineE3 ubiquitin ligaseInhibitorinhibitorinhibit

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