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Cat. No.: HY-117222

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AM-0216

AM-0216 is a selective NIK inhibitor (K_i 2.0 nM) that acts on the non-canonical NF‑κB signaling pathway. AM‑0216 selectively inhibits NIK-dependent NF‑κB activation, reduces RelB:p52 activity, and inhibits BAFF receptor-induced NF‑κB activity. AM‑0216 induces apoptosis and NIK-dependent cytotoxicity in myeloma cells, inhibits cell clonogenic formation, and suppresses tumor growth in B-cell malignancies with constitutive NIK activation. AM-0216 can be used for research on mantle cell lymphoma, multiple myeloma, and B-cell malignancies.

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

CAS No.: 1202764-61-1
Formula: C₁₉H₁₇N₅OS
Molecular Weight:363.44

Storage:

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

Data Sheet (275 KB)

AM-0216 Chemical Structure

CAS No.: 1202764-61-1

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

NF-κB

All NF-κB Isoforms :

In Vitro

Anti-cancerApoptosisOthers

Anti-cancer

AM-0216 combined with CC-292 (HY-18012) produces a significant synergistic effect in relapsed/refractory mantle cell lymphoma cell lines, achieving complete inhibition of the NFKB pathway^[1].
AM-0216 reduces RelB:p52 activity and inhibits tumor growth in B-cell malignancies with constitutive NIK activation^[4].

Anti-cancer

Apoptosis

AM-0216 (1-5 μM) effectively inhibits NIK-dependent NF-κB activation in multiple myeloma cell lines carrying mutations in alternative NF-κB pathway components and downregulates the mRNA levels of NF-κB target genes; it inhibits BAFF receptor-induced NF-κB activity in MM-S1 cells, induces cytotoxicity and apoptosis in NIK-activated multiple myeloma cell lines, and prevents colony formation^[2].

Others

AM-0216 inhibits NIK with a K_i of 2 nM in biochemical HTRF assays^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Chemical Information

CAS No. 1202764-61-1
Molecular Weight 363.44
Formula C₁₉H₁₇N₅OS
SMILES

C(#C[C@@](C)(O)C1=NC=CS1)C=2C=C3N(CCC3=CC2)C4=NC(N)=NC=C4
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 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]. Sarkozy C, et al. Novel agents for mantle cell lymphoma: molecular rational and clinical data. Expert Opinion on Investigational Drugs. 2020 Jun 2;29(6):555-66.

[2]. Maubach G, et al. NF-kappaB-inducing kinase in cancer. Biochimica et Biophysica Acta (BBA)-Reviews on Cancer. 2019 Jan 1;1871(1):40-9.

[3]. Ren X, et al. A small-molecule inhibitor of NF-κB-inducing kinase (NIK) protects liver from toxin-induced inflammation, oxidative stress, and injury. FASEB journal : official publication of the Federation of American Societies for Experimental Biology. 2017 Feb;31(2):711-718. [Content Brief]

[4]. Hoffmann A, et al. NF-κB: master regulator of cellular responses in health and disease. Immunity & inflammation. 2025;1(1):2.

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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.

Bioz

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100 mg

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Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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AM-0216

All NF-κB Isoforms