2. PROTAC MAPK/ERK Pathway
  3. PROTACs Mixed Lineage Kinase
  4. PROTAC MLKL Degrader-3

PROTAC MLKL Degrader-3 (compound C116) 是一种 MLKL PROTAC 降解剂。PROTAC MLKL Degrader-3 可通过泛素化作用诱导依赖蛋白酶体和 cereblon 的 MLKL 降解。PROTAC MLKL Degrader-3 可用于肝细胞癌的研究。
(粉色: Mixed Lineage Kinase 配体 (HY-182344)；蓝色: Cereblon 配体 (HY-14658)；黑色: 连接子)。

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PROTAC MLKL Degrader-3

PROTAC MLKL Degrader-3 Chemical Structure

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PROTAC MLKL Degrader-3 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC MLKL Degrader-3 (compound C116) is a MLKL PROTAC degrader. PROTAC MLKL Degrader-3 induces proteasome- and cereblon-dependent MLKL degradation via ubiquitination. PROTAC MLKL Degrader-3 is applicable to the research of hepatocellular carcinoma[1]. (Pink: Mixed Lineage Kinase ligand (HY-182344); Blue: Cereblon ligand (HY-14658); Black: linker).

体外研究
(In Vitro)

PROTAC MLKL Degrader-3 (compound C116) (1 nM-20000 nM, 0.5 μM-1 μM; 2 h-96 h) 可强效且快速地降解小鼠 Hepa1-6 细胞和人 HepG2 肝癌 (HCC) 细胞中的 MLKL，两种细胞系对应的 DC50 值分别为 248.9 nM 和 271.3 nM，最大降解率均超过 90%[1]。
PROTAC MLKL Degrader-3 (C116) (1 μM; 4 h) 可在小鼠 Hepa1-6 肝癌细胞中选择性降解 MLKL，而不会显著影响蛋白质组中的其他蛋白质[1]。
PROTAC MLKL Degrader-3 (C116) (孵育 6 h) 可通过增强小鼠 Hepa1-6 细胞和人 HEK293T 细胞中 MLKL 的泛素化水平，以蛋白酶体和 CRBN 依赖的方式介导 MLKL 降解[1]。
PROTAC MLKL Degrader-3 (C116) (1 μM-10 μM; 24 h pretreatment, followed by 20 h PA stimulation) 可增强 PA 诱导的小鼠 Hepa1-6 细胞和人 HepG2 肝癌细胞的 PARP 依赖性细胞死亡 (parthanatos) 及后续细胞毒性，且该效应依赖于 PARP 依赖性细胞死亡信号通路[1]。
PROTAC MLKL Degrader-3 (C116) 可在多种小鼠和人类癌细胞系中降解 MLKL，包括结直肠癌、三阴性乳腺癌和肺癌细胞[1]。

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

PROTAC MLKL Degrader-3 相关抗体:

Western Blot Analysis[1]

Cell Line: murine Hepa1-6 HCC cells, human HepG2 HCC cells
Concentration: 1 μM, 10 μM (24 h); 1 nM-20000 nM (24 h); 0.5 μM, 1 μM (2 h, 4 h, 6 h, 12 h, 24 h, 48 h, 72 h, 96 h)
Incubation Time: 24 h (1 μM, 10 μM, 1 nM-20000 nM); 2 h-96 h (0.5 μM, 1 μM)
Result: Reduced MLKL levels to 9.6% in Hepa1-6 cells and 18.7% in HepG2 cells at 1 μM for 24 h.
Reduced MLKL levels to 2.5% in Hepa1-6 cells and 11.7% in HepG2 cells at 10 μM for 24 h.
Induced concentration-dependent degradation with DC50 values of 248.9 nM in Hepa1-6 cells and 271.3 nM in HepG2 cells, and maximal percent degradation (Dₘₐₓ) of 99.3% in Hepa1-6 cells and 91.2% in HepG2 cells.
Induced over 90% MLKL reduction as early as 2 h at 1 μM, with robust degradation maintained for 48 h and recovery observed by 96 h.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUC
Mice[1] 10 mg/kg i.p. 5.5 h 1519 ng·h/mL
体内研究
(In Vivo)

PROTAC MLKL Degrader-3 (compound C116) (10 mg/kg；腹腔注射；每日给药) 可显著降低雄性 C57BL/6 小鼠的瘤内 MLKL 水平，并抑制原位 HCC 肿瘤生长，且耐受性良好[1]。

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

Animal Model: C57BL/6 (male, 5 weeks old, orthotopic liver tumor model via surgical implantation of Hepa1−6-luc cells)[1]
Dosage: 10 mg/kg
Administration: i.p.; daily; study duration
Result: Significantly inhibited orthotopic HCC tumor growth, as measured by reduced total bioluminescent flux.
Significantly reduced intratumoral MLKL levels in treated mice.
Showed good tolerability, with no induced weight loss in treated mice.
分子量

1026.02

Formula

C49H47F4N11O8S
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 MLKL Degrader-3 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

PROTAC MLKL Degrader-3PROTAC MLKL Degrader3PROTAC MLKL Degrader 3PROTACsMixed Lineage KinaseMLKsproteasomecereblonpoly(ADP-ribose) polymerHepG2parthanatosmixed lineage kinase domain-like pseudokinasehepatocellular carcinomaHepa1-6MLKLapoptosis-inducing factorInhibitorinhibitorinhibit

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产品名称：
PROTAC MLKL Degrader-3
目录号：
HY-182343
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