ACHP

Cat. No.: HY-107592: FAQs
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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.

For research use only. We do not sell to patients.

ACHP Chemical Structure

CAS No. : 406208-42-2

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Other In-stock Forms of ACHP:

ACHP Hydrochloride

Other Forms of ACHP:

ACHP Hydrochloride In-stock

8 Publications Citing Use of MCE ACHP

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IKK-α IKK-β IKK IKKε TBK1

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STAT3 STAT5 STAT6 STAT1

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

IKK-β

8.5 nM (IC₅₀)

IKK-α

250 nM (IC₅₀)

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]

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.

Molecular Weight

364.44

Formula

C₂₁H₂₄N₄O₂

CAS No.

406208-42-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

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]

ACHP Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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