Cat. No.: HY-107592

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ACHP

Name: ACHP
Brand: MedChemExpress
SKU: HY-107592
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10 Cited Publications

고객리뷰

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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CAS No.: 406208-42-2
화학식: C₂₁H₂₄N₄O₂
분자량:364.44

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (280 KB)

ACHP Chemical Structure

CAS No.: 406208-42-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (10)
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

IKK-β

8.5 nM (IC₅₀)

IKK-α

250 nM (IC₅₀)

All IKK Isoforms :

All STAT Isoforms :

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]
HEK293	IC₅₀	130 nM Compound: 4j	Tested for TNF-alpha-induced NF-KB transactivation in HEK293 cells Tested for TNF-alpha-induced NF-KB transactivation in HEK293 cells	[PMID: 15225718]
HUVEC	IC₅₀	30 nM Compound: 4j	Tested for TNF-alpha-induced VCAM-1 production in HUVECS cells Tested for TNF-alpha-induced VCAM-1 production in HUVECS cells	[PMID: 15225718]
Jurkat	IC₅₀	147 nM Compound: 4j	Tested for PMA/Ca-induced NF-KB transactivation in Jurkat T-cells Tested for PMA/Ca-induced NF-KB transactivation in Jurkat T-cells	[PMID: 15225718]
Jurkat	IC₅₀	10 μM Compound: 4j	Tested for PMA/Ca-induced NF-AT transactivation in Jurkat T-cells Tested for PMA/Ca-induced NF-AT transactivation in Jurkat T-cells	[PMID: 15225718]
PBMC	IC₅₀	45 nM Compound: 4j	Tested for LPS induced IL-6 production in human PBMC cells Tested for LPS induced IL-6 production in human PBMC cells	[PMID: 15225718]
PBMC	IC₅₀	50 nM Compound: 4j	Tested for LPS induced TNFalpha production in human PBMC cells Tested for LPS induced TNFalpha production in human PBMC cells	[PMID: 15225718]
PBMC	IC₅₀	96 nM Compound: 4j	Tested for LPS induced IL1-beta production in human PBMC cells Tested for LPS induced IL1-beta production in human PBMC cells	[PMID: 15225718]

In Vitro

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.

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.

In Vivo

ACHP (0.3, 1, 3 mg/kg; p.o.; single) exhibits anti-inflammatory activity in Arachidonic acid-induced ear edema mice model^[3].

MedChemExpress (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.

Related Protocols :

Chemical Information

CAS No. 406208-42-2
분자량 364.44
화학식 C₂₁H₂₄N₄O₂
SMILES

NC1=NC(C(C(O)=CC=C2)=C2OCC3CC3)=CC(C4CCNCC4)=C1C#N
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (10)

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Journal Impact Factor

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

STING-NF-κB signaling builds an influenza spillover barrier. [Abstract]

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

Enhanced Tendon-to-Bone Healing via IKKβ Inhibition in a Rat Rotator Cuff Model. [Abstract]

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
University of Bonn

2025.
Patent

US20190248778A1.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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ACHP

Publications Citing Use of MedChemExpress (MCE) ACHP

All IKK Isoforms

All STAT Isoforms