2. PROTAC Epigenetics Apoptosis Cell Cycle/DNA Damage
  3. PROTACs Histone Demethylase Apoptosis Caspase PARP
  4. YTHu78

YTHu78 是一种 KDM5B PROTAC 类降解剂。YTHu78 通过泛素-蛋白酶体系统诱导 KDM5B 降解，并在 MV-4-11 和 MM.1S 细胞系中引发细胞凋亡 (apoptosis)。YTHu78 对多种血液肿瘤细胞系表现出显著的抗增殖活性，可用于研究血液肿瘤。(粉色： GSK467 配体： (HY-116761); 蓝色： Thalidomide 配体： (HY-14658), 黑色 + 粉色： GSK467 配体+linker： (HY-175145))。

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YTHu78

YTHu78 Chemical Structure

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Customer Review

YTHu78 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Histone Demethylase 亚型特异性产品:

查看所有亚型
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

查看 Caspase 亚型特异性产品:

查看所有亚型
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

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YTHu78 is a KDM5B PROTAC-type degrader. YTHu78 induces KDM5B degradation via the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 exhibits significant antiproliferative activity against a variety of hematological cancer cell lines and can be used to study hematological cancers. (Pink: KDM5B ligand: (HY-116761); Blue: Thalidomide ligand: (HY-14658), Black + Pink: KDM5B ligand + linker: (HY-175145))[1].

IC50 & Target[1]

Cereblon

 

KDM5B

 

Caspase 3

 

体外研究
(In Vitro)

YTHu78 (72 小时) 对 MV-4-11、HL60、MM.1S 和 OCI-AML3 细胞表现出抗增殖活性，IC50 分别为 1.34 μM、6.58 μM、1.03 μM 和 9.07 μM[1]。

YTHu78 (0.03-20 μM, 1-24 小时) 通过蛋白酶体介导的途径降低 MV-4-11 和 MM.1S 细胞中的 KDM5B 蛋白水平[1]。

YTHu78 (0.03-20 μM, 48 小时) 诱导 MV-4-11 和 MM.1S 细胞中依赖 caspase 的溶解性细胞凋亡[1]。

YTHu78 (72 小时) 对原代 HUVEC、GM00637 成纤维细胞、HaCaT 角质形成细胞、GES-1 和 HEK293 细胞均表现出可忽略不计的抗增殖作用，IC50 均 > 20 μM[1]。

YTHu78 (72 小时) 对难治性实体瘤和中等敏感实体瘤模型表现出有限的抗增殖作用，包括 HCC、PDAC、gGBM 和 TNBC 细胞,，IC50 >20 μM，对 Huh-7、HCC1937 和 PANC-1 细胞的 IC50 为 6-20 μM[1]。

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

YTHu78 相关抗体:

Western Blot Analysis[1]

Cell Line: MV-4-11 cells, MM.1S cells
Concentration: 0.03 μM, 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 5 μM, 6.7 μM, 20 μM
Incubation Time: 1 h, 3 h, 6 h, 12 h, 24 h,48 h
Result: Induced KDM5B protein degradation at a concentration of 0.74 μM and depleted KDM5B in a time-dependent manner, with maximal degradation achieved after 12 hours of treatment at a concentration of 5 μM.
Increased H3K4me3 levels.
Activated Caspase-3, induced PARP cleavage, and upregulated cleaved-GSDMD and cleaved-GSDME after 48 h of 5 μM treatment.

RT-PCR[1]

Cell Line: MV-4-11 cells, MM.1S cells
Concentration: 0.03 μM, 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 5 μM, 6.7 μM, 20 μM
Incubation Time: 24 h
Result: Did not affect KDM5B mRNA levels at low doses, increased mRNA levels at high concentrations in MM.1S cells.

Apoptosis Analysis[1]

Cell Line: MV-4-11 cells, MM.1S cells
Concentration: 0.03 μM, 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 5 μM, 6.7 μM, 20 μM
Incubation Time: 48 h
Result: Increased apoptotic population, induced mild G0/G1 cell cycle arrest at high doses, and increased LDH release.
分子量

632.63

Formula

C33H28N8O6
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

YTHu78 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 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

YTHu78YTHu 78YTHu-78PROTACsHistone DemethylaseApoptosisCaspasePARPpoly ADP ribose polymeraseDegraderHematologic malignanciesMV-4-11 cellsMM.1S cellsInhibitorinhibitorinhibit

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