1. Cell Cycle/DNA Damage
  2. CDK Wee1 Checkpoint Kinase (Chk)
  3. DHI1

DHI1 是一种抗白血病剂并且对 Jurkat (IC50 = 21.83 μM) 和 HL-60 (IC50 = 19.14 μM) 白血病细胞具有高选择性,对非癌细胞具有低毒性。DHI1 诱导 Jurkat 和 HL-60 白血病细胞 G2/M 细胞周期停滞和 HL-60 细胞的 S 期停滞,对细胞周期信号分子 Wee1, cyclin B1, cdc2 on Tyr15, Chk1 有明显影响。DHI1 通过破坏细胞骨架肌动蛋白丝来抑制 Jurkat 和 HL-60 细胞的迁移和侵袭性。DHI1 可用于研究血液恶性肿瘤。

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DHI1

DHI1 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DHI1 is an anti-leukemia agent with high selectivity for Jurkat (IC50 = 21.83 μM) and HL-60 (IC50 = 19.14 μM) leukemia cells and has low toxicity to non-cancerous cells. DHI1 can induce G2/M phase cell arrest in Jurkat and HL-60 leukemia cells, as well as S phase arrest in HL-60 cells, and has significant effects on cell cycle signaling molecules Wee1, cyclin B1, cdc2 on Tyr15, and Chk1. DHI1 inhibits the migration and invasion of Jurkat and HL-60 cells by disrupting cytoskeletal actin filaments. DHI1 can be used to study hematological malignancies[1].

IC50 & Target[1]

Chk1

 

体外研究
(In Vitro)

DHI1 (Compound 4a) (3-100 μM,24-72 小时) 对 Jurkat 和 HL-60 细胞表现出抑制作用,IC50 分别为 21.83 和 19.14 μM,但对 HCT-116、HeLa、MCF-7、U87、Hep G2、A549、A2780、BJ-5ta 和 MCF-10A 细胞的抑制作用较弱[1]
DHI1 (19.14-21.83 μM,24-72 小时) 在 Jurkat 和 HL-60 细胞中诱导细胞周期停滞于 G2/M 期,并影响与细胞周期相关的信号蛋白[1]
DHI1 (10-40 μM,3 小时) 降低 Jurkat 和 HL-60 白血病细胞的趋化性和侵袭性[1]
DHI1 (19.14-21.83 μM,24-72 小时) 在 Jurkat 和 HL-60 白血病细胞中可诱导 F- 肌动蛋白结构破坏、紊乱、损伤,以及核碎裂和膜起泡,影响细胞骨架[1]
DHI1 (3.125-100 μM,24 小时) 可增强 PBMC 细胞活力[1]

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

Cell Cycle Analysis[1]

Cell Line: Jurkat cells
Concentration: 21.83 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Induced cell cycle arrest at G2/M phase at 24 h and increases sub-G0/G1 fraction. Reduced phosphorylation of Wee1 (Ser642) , cyclin B1 (Ser133), cdc2 on Tyr15, human retinoblastoma protein (Rb) .
Increased phosphorylation of Chk1 (Ser345), but reduced phosphorylation of Chk1 (Ser345) after 72 hours.
Increased the level of p21 at 24 and 48 h.

Cell Cycle Analysis[1]

Cell Line: HL-60 cells
Concentration: 19.14 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Induced cell cycle arrest at G2/M phase after 24 h, blocked S phase, and increased sub-G0/G1 peak of DNA fragmentation.
Reduced phosphorylation of Wee1 (Ser642), cdc2 on Tyr15, human retinoblastoma protein (Rb), increased phosphorylation of Chk1 (Ser345).
Increased the level of p21 at 24 h, but decrease p21 at 48-72 h.

Cell Migration Assay [1]

Cell Line: Jurkat and HL-60 cells
Concentration: 10, 20, and 40 μM
Incubation Time: 3 h
Result: Decreased relative cell chemotaxis by 31.1 and 45.7% at 40 μM, reduced HL-60 cell invasion by 17.7% at 20 μM.
Induced concentration-dependent effects on the invasiveness/motility, reduced cell invasion by 39.7 and 57.8% at 40 μM, reduced HL-60 cell invasion by 33.6% at 20 μM.
分子量

355.23

Formula

C18H15BrN2O

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
  • 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)

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.

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DHI1
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HY-175261
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