2. NF-κB Stem Cell/Wnt JAK/STAT Signaling Apoptosis
  3. IKK STAT Apoptosis
  4. ACHP

ACHP (化合物 4j) 是一种选择性和口服有效的 IκB 激酶抑制剂，其对 IKKβ 和 IKKαIC50 值分别为 8.5 nM 和250 nM。ACHP 能有效抑制 STAT3 信号通路并诱导癌细胞周期停滞和凋亡 (apoptosis)。ACHP 在小鼠耳水肿模型中具有抗炎活性。ACHP 可用于抗炎和抗癌 (如多发性骨髓瘤和白血病) 的研究。

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ACHP Chemical Structure

ACHP Chemical Structure

CAS No. : 406208-42-2

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100 mg   询价  
250 mg   询价  

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ACHP 的其他形式现货产品:

Customer Review

Other Forms of ACHP:

ACHP 相关抗体

Top Publications Citing Use of Products

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IKK-α IKK-β IKK IKKε TBK1

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies[1][2][3][4].

IC50 & Target[1]

IKK-β

8.5 nM (IC50)

IKK-α

250 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
40 nM
Compound: 4j
TNF-alpha-induced RANTES production in A549 cells using ELISA assay
TNF-alpha-induced RANTES production in A549 cells using ELISA assay
[PMID: 15225718]
体外研究
(In Vitro)

ACHP (0-100 µM; 3 days) 抑制骨髓瘤细胞系 (U266, NCUMM-2, ILKM-2) 生长的平均 IC50 值为 26.8 µM[1]。
ACHP (10 µM; 24 h) 诱导 U266 和 NCUMM-2 细胞周期停滞[1]。
ACHP (10, 50 µM; 8 h) 诱导 NCUMM-2 细胞凋亡[1]。
ACHP (0-50 µM; 20 min) 在 MT-2 and ED-40515(-) 细胞中抑制 IkBa 和 p65 的磷酸化[2]。

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

ACHP 相关抗体:

Cell Viability Assay[1]

Cell Line: U266, NCUMM-2, ILKM-2
Concentration: 0-100 µM
Incubation Time: 3 days
Result: Inhibited the growth of myeloma cell lines in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: U266 and NCUMM-2 cells
Concentration: 10 µM
Incubation Time: 24 h
Result: Caused cell cycle arrest in the G1 phase.

Apoptosis Analysis[1]

Cell Line: NCUMM-2 cells
Concentration: 10, 50 µM
Incubation Time: 8 h
Result: Efficiently induced apoptosis in 15.8%, 43.7% at a concentration of 10 and 50 µM, respectively.

Western Blot Analysis[2]

Cell Line: MT-2 and ED-40515(-) cells
Concentration: 0-50 µM
Incubation Time: 20 min
Result: Inhibited phosphorylation of IkBa and p65 with IC50 values in MT-2 cells were 0.4 and 0.2 µM, respectively.
Inhibited phosphorylation of IkBa and p65 with IC50 values in ED-40515 (-) cells were 10.2 and 29.5 µM, respectively.
体内研究
(In Vivo)

ACHP (0.3, 1, 3 mg/kg; p.o.; single) 在 Arachidonic acid 诱导的耳水肿小鼠模型中显示出抗炎活性[3]。

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

Animal Model: Arachidonic acid-induced ear edema mice model[3].
Dosage: 0.3, 1, 3 mg/kg
Administration: Oral administration; single
Result: Showed anti-inflammatory activity in a dose-dependent manner.
分子量

364.44

Formula

C21H24N4O2
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

ACHP 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:

ACHP406208-42-2IKKSTATApoptosisIκB kinaseI kappa B kinase ILKM-2ILKM-3KM5U266NCUMM-2AMO1NOP1cancerapoptosistumorinflammationInhibitorinhibitorinhibit

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