ACHP
Based on 10 publication(s) in Google Scholar
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.
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- No. CAS: 406208-42-2
- Fòrmula: C21H24N4O2
- Peso molecular:364.44
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ACHP
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Science. 2026 Feb 26;391(6788):eads4405. [Abstract]
- Nat Commun. 2020 Jul 9;11(1):3427. [Abstract]
- Cell Death Dis. 2020 Oct 15;11(10):863. [Abstract]
- J Bone Miner Res. 2019 Oct;34(10):1880-1893. [Abstract]
- Am J Sports Med. 2021 Mar;49(3):780-789. [Abstract]
- Sci Rep. 2021 Jul 28;11(1):15319. [Abstract]
- J Orthop Res. 2023 Oct;41(10):2295-2304. [Abstract]
- University of Bonn. 2025.
- Patent. US20190248778A1.
Actividad biológica
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IKK-β 8.5 nM (IC50) |
IKK-α 250 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
40 nM
Compound: 4j
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TNF-alpha-induced RANTES production in A549 cells using ELISA assay
TNF-alpha-induced RANTES production in A549 cells using ELISA assay
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[PMID: 15225718] |
| HEK293 | IC50 |
130 nM
Compound: 4j
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Tested for TNF-alpha-induced NF-KB transactivation in HEK293 cells
Tested for TNF-alpha-induced NF-KB transactivation in HEK293 cells
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[PMID: 15225718] |
| HUVEC | IC50 |
30 nM
Compound: 4j
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Tested for TNF-alpha-induced VCAM-1 production in HUVECS cells
Tested for TNF-alpha-induced VCAM-1 production in HUVECS cells
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[PMID: 15225718] |
| Jurkat | IC50 |
147 nM
Compound: 4j
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Tested for PMA/Ca-induced NF-KB transactivation in Jurkat T-cells
Tested for PMA/Ca-induced NF-KB transactivation in Jurkat T-cells
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[PMID: 15225718] |
| Jurkat | IC50 |
10 μM
Compound: 4j
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Tested for PMA/Ca-induced NF-AT transactivation in Jurkat T-cells
Tested for PMA/Ca-induced NF-AT transactivation in Jurkat T-cells
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[PMID: 15225718] |
| PBMC | IC50 |
45 nM
Compound: 4j
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Tested for LPS induced IL-6 production in human PBMC cells
Tested for LPS induced IL-6 production in human PBMC cells
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[PMID: 15225718] |
| PBMC | IC50 |
50 nM
Compound: 4j
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Tested for LPS induced TNFalpha production in human PBMC cells
Tested for LPS induced TNFalpha production in human PBMC cells
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[PMID: 15225718] |
| PBMC | IC50 |
96 nM
Compound: 4j
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Tested for LPS induced IL1-beta production in human PBMC cells
Tested for LPS induced IL1-beta production in human PBMC cells
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[PMID: 15225718] |
ACHP (0-100 µM; 3 days) inhibits cell growth with mean IC50 of 26.8 µM in three myeloma cell lines (U266, NCUMM-2, ILKM-2)[1].
ACHP (10 µM; 24 h) induces cycle arrest in U266 and NCUMM-2 cells[1].
ACHP (10, 50 µM; 8 h) induces apoptosis in NCUMM-2 cells[1].
ACHP (0-50 µM; 20 min) inhibits the phosphorylation of IkBa and p65 in MT-2 and ED-40515(-) cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U266, NCUMM-2, ILKM-2
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Concentration:0-100 µM
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Incubation Time:3 days
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Result:Inhibited the growth of myeloma cell lines in a dose-dependent manner.
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Cell Line:U266 and NCUMM-2 cells
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Concentration:10 µM
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Incubation Time:24 h
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Result:Caused cell cycle arrest in the G1 phase.
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Cell Line:NCUMM-2 cells
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Concentration:10, 50 µM
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Incubation Time:8 h
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Result:Efficiently induced apoptosis in 15.8%, 43.7% at a concentration of 10 and 50 µM, respectively.
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Cell Line:MT-2 and ED-40515(-) cells
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Concentration:0-50 µM
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Incubation Time:20 min
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Arachidonic acid-induced ear edema mice model[3].
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Dosage:0.3, 1, 3 mg/kg
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Administration:Oral administration; single
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Result:Showed anti-inflammatory activity in a dose-dependent manner.
Chemical Information
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No. CAS 406208-42-2
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Peso molecular 364.44
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Fòrmula C21H24N4O2
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SMILES
NC1=NC(C(C(O)=CC=C2)=C2OCC3CC3)=CC(C4CCNCC4)=C1C#N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (10)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Science
2026 Feb 26;391(6788):eads4405. PMID: 41747053 -
Nat Commun
LDHA-mediated ROS generation in chondrocytes is a potential therapeutic target for osteoarthritis. [Abstract]2020 Jul 9;11(1):3427. PMID: 32647171 -
Cell Death Dis
Mesenchymal stem cells reverse EMT process through blocking the activation of NF-κB and Hedgehog pathways in LPS-induced acute lung injury. [Abstract]2020 Oct 15;11(10):863. PMID: 33060560 -
J Bone Miner Res
Attenuation of NF-κB in Intestinal Epithelial Cells Is Sufficient to Mitigate the Bone Loss Comorbidity of Experimental Mouse Colitis. [Abstract]2019 Oct;34(10):1880-1893. PMID: 31107556 -
Am J Sports Med
2021 Mar;49(3):780-789. PMID: 33507808 -
Sci Rep
A phenotypic high-content, high-throughput screen identifies inhibitors of NLRP3 inflammasome activation. [Abstract]2021 Jul 28;11(1):15319. PMID: 34321581 -
J Orthop Res
The effects of NF-κB suppression on the early healing response following intrasynovial tendon repair in a canine model. [Abstract]2023 Oct;41(10):2295-2304. PMID: 37094977 -
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Pureza y Documentación
Referencias
[1]. Sanda T, et al. Growth inhibition of multiple myeloma cells by a novel IkappaB kinase inhibitor. Clin Cancer Res. 2005 Mar 1;11(5):1974-82. [Content Brief]
[2]. Lee JH, et al. The IκB Kinase Inhibitor ACHP Targets the STAT3 Signaling Pathway in Human Non-Small Cell Lung Carcinoma Cells. Biomolecules. 2019 Dec 13;9(12):875. [Content Brief]
[3]. Murata T, et al. Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents. Bioorg Med Chem Lett. 2004 Aug 2;14(15):4019-22. [Content Brief]
[4]. Sanda T, et al. Induction of cell death in adult T-cell leukemia cells by a novel IkappaB kinase inhibitor. Leukemia. 2006 Apr;20(4):590-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ACHP Related Classifications
HY-107592 Related Classifications
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