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Cat. No.: HY-124069

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M-525

M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC₅₀ of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity.

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

CAS No.: 2173582-08-4
Formula: C₃₉H₅₁FN₆O₅S
Molecular Weight:734.92

Storage:

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

Data Sheet (266 KB)

M-525 Chemical Structure

CAS No.: 2173582-08-4

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Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	GI₅₀	0.9 μM Compound: 9; M-525	Anticancer activity against human HL-60 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay Anticancer activity against human HL-60 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 36528996]
HL-60	IC₅₀	1500 nM Compound: M-525	Growth inhibition of human HL60 cells after 7 days by WST-8 assay Growth inhibition of human HL60 cells after 7 days by WST-8 assay	[PMID: 32338903]
K562	GI₅₀	0.9 μM Compound: 9; M-525	Anticancer activity against human K562 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay Anticancer activity against human K562 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 36528996]
MOLM-13	GI₅₀	15.4 nM Compound: 15; M-525	Antiproliferative activity against human MOLM-13 cells Antiproliferative activity against human MOLM-13 cells	[PMID: 34726905]
MOLM-13	GI₅₀	2.3 nM Compound: 9; M-525	Anticancer activity against human MOLM-13 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay Anticancer activity against human MOLM-13 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 36528996]
MOLM-13	IC₅₀	19 nM Compound: M-525	Growth inhibition of human MOLM13 cells after 7 days by WST-8 assay Growth inhibition of human MOLM13 cells after 7 days by WST-8 assay	[PMID: 32338903]
MOLM-14	GI₅₀	2.3 nM Compound: 9; M-525	Anticancer activity against human MOLM-14 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay Anticancer activity against human MOLM-14 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 36528996]
MOLM-16	GI₅₀	0.9 μM Compound: 9; M-525	Anticancer activity against human MOLM16 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay Anticancer activity against human MOLM16 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 36528996]
MONO-MAC-6	GI₅₀	2.3 nM Compound: 9; M-525	Anticancer activity against human MONO-MAC-6 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay Anticancer activity against human MONO-MAC-6 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 36528996]
MV4-11	GI₅₀	2.3 nM Compound: 9; M-525	Anticancer activity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay Anticancer activity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 36528996]
MV4-11	GI₅₀	2.7 nM Compound: 15; M-525	Antiproliferative activity against human MV4-11 cells Antiproliferative activity against human MV4-11 cells	[PMID: 34726905]
MV4-11	IC₅₀	4 nM Compound: M-525	Growth inhibition of human MV4-11 cells after 7 days by WST-8 assay Growth inhibition of human MV4-11 cells after 7 days by WST-8 assay	[PMID: 32338903]
RS4-11	GI₅₀	2.3 nM Compound: 9; M-525	Anticancer activity against human RS4-11 cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay Anticancer activity against human RS4-11 cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 36528996]
SEM	GI₅₀	2.3 nM Compound: 9; M-525	Anticancer activity against human SEM cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay Anticancer activity against human SEM cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 36528996]
SKM-1	GI₅₀	0.9 μM Compound: 9; M-525	Anticancer activity against human SKM-1 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay Anticancer activity against human SKM-1 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 36528996]

In Vitro

M-525 achieves an IC₅₀ of 3 nM in the MV4;11 cell line and has an IC₅₀ of 2 µM in the HL-60 cell line. M-525 (3-300 nM; 24 h) is potent and effective in suppressing the expression of MEIS1 and HOX genes in MV4;11 cells carrying the MLL-AF4 fusion and in MOLM-13 cells carrying the MLL-AF9 fusion. It demonstrates high cellular specificity over non-MLL leukemia cells^[1].

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

Chemical Information

CAS No. 2173582-08-4
Molecular Weight 734.92
Formula C₃₉H₅₁FN₆O₅S
SMILES

O=C(OC)N[C@@H]1[C@@H]([C@](C2CCN(CC3CN(C4=CC=C(S(=O)(C5CN(C(/C=C/CN(C)C)=O)C5)=O)C=C4)C3)CC2)(C#N)C6=CC=CC(F)=C6)CCC1
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 (266 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]. Xu S, et al. Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction. Angew Chem Int Ed Engl. 2018 Feb 5;57(6):1601-1605. [Content Brief]

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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.

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100 mg

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

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M-525

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

M-525 Related Classifications

HY-124069 Related Classifications