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

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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ACHP

ACHP 화학구조

CAS No. : 406208-42-2

사이즈 재고
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Other Forms of ACHP:

ACHP Related Antibodies

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  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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)

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
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]
Jurkat IC50
10000 nM
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]
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]
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.

ACHP Related Antibodies

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.
분자량

364.44

화학식

C21H24N4O2
CAS No.
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.
순도&문서
References
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ACHP Related Classifications

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  • 농도 희석 계산기

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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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상품명:
ACHP
Cat. No.:
HY-107592
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