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Chemical Structure| 406209-26-5 Chemical Structure| 406209-26-5

Structure of ACHP HCl
CAS No.: 406209-26-5

Chemical Structure| 406209-26-5

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ACHP HCl is a potent and selective IKK-2 inhibitor with IC50 of 8.5 nM.

Synonyms: IKK-2 Inhibitor VIII; ACHP Hydrochloride

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Product Details of ACHP HCl

CAS No. :406209-26-5
Formula : C21H25ClN4O2
M.W : 400.90
SMILES Code : N#CC1=C(N)N=C(C2=C(O)C=CC=C2OCC3CC3)C=C1C4CCNCC4.[H]Cl
Synonyms :
IKK-2 Inhibitor VIII; ACHP Hydrochloride
MDL No. :MFCD22124458

Safety of ACHP HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of ACHP HCl

pyroptosis
TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
human keratinocytes 2.5 μM 30 min Inhibited NF-κB signaling pathway, reduced induction of CXCL8, CXCL1, and CXCL2 J Invest Dermatol. 2019 Jul;139(7):1506-1515. e7
mouse keratinocytes 2.5 μM 30 min Inhibited NF-κB signaling pathway, prevented IκBα degradation, and reduced induction of pro-inflammatory cytokines and chemokines J Invest Dermatol. 2019 Jul;139(7):1506-1515. e7
Human adult lung fibroblasts (HLFa) 50 μM 24 h To investigate the inhibitory effect of ACHP on TGF-β1-induced fibroblast-to-myofibroblast transition. Results showed that ACHP significantly suppressed the expression of αSMA and SM22α, as well as the deposition of collagen type I and fibronectin. J Cell Mol Med. 2015 Dec;19(12):2780-92
HEL 299 cells 1-30 µM 24 h Concentration-dependent reduction in cell viability Biomolecules. 2019 Dec 13;9(12):875
H1299 cells 10 µM 4 h Inhibited IL-6-induced STAT3 activation, reduced phosphorylation of upstream kinases JAK1, JAK2, and Src Biomolecules. 2019 Dec 13;9(12):875
A549 cells 10 µM 4 h Inhibited STAT3 phosphorylation, reduced STAT3 nuclear translocation and DNA binding ability Biomolecules. 2019 Dec 13;9(12):875
human dendritic cells 500 nM 24 h Inhibition of NF-κB signaling pathway, significantly inhibited IDO1 biosynthesis PLoS One. 2015 Feb 25;10(2):e0118562
OM10.1 cells 0.56 μM 24 h To evaluate the inhibitory effect of ACHP on TNF-α-induced HIV-1 replication. Results showed that ACHP significantly inhibited the increase in HIV p24 antigen levels, with an EC50 of approximately 0.56 μM. Antimicrob Agents Chemother. 2006 Feb;50(2):547-55

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice K5-PKCα transgenic mice Topical application 5 mg/kg 30 minutes pretreatment Reduced skin inflammation and tumor formation, inhibited UV and IMQ-induced inflammation J Invest Dermatol. 2019 Jul;139(7):1506-1515. e7

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.49mL

0.50mL

0.25mL

12.47mL

2.49mL

1.25mL

24.94mL

4.99mL

2.49mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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