DX2-201

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DX2-201 is a potent and selective oxidative phosphorylation (OXPHOS) complex I inhibitor with an IC₅₀ of 312 nM. DX2-201 has anticancer effects.

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DX2-201 Chemical Structure

CAS No. : 2749554-00-3

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Description

DX2-201 is a potent and selective oxidative phosphorylation (OXPHOS) complex I inhibitor with an IC₅₀ of 312 nM. DX2-201 has anticancer effects^[1].

IC₅₀ & Target

IC50: 312 nM (OXPHOS complex I)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	0.6 μM Compound: 2; DX2-201	Cytotoxicity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 7 days in glucose-containing medium by MTT assay Cytotoxicity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 7 days in glucose-containing medium by MTT assay	[PMID: 34982568]
MIA PaCa-2	IC₅₀	> 10 μM Compound: 2; DX2-201	Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 3 days in galactose-containing medium by MTT assay Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 3 days in galactose-containing medium by MTT assay	[PMID: 34982568]
MIA PaCa-2	IC₅₀	0.09 μM Compound: 2; DX2-201	Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 3 days in glucose-containing medium by MTT assay Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 3 days in glucose-containing medium by MTT assay	[PMID: 34982568]
MIA PaCa-2	IC₅₀	0.4 μM Compound: 2; DX2-201	Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 7 days in glucose-containing medium by MTT assay Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 7 days in glucose-containing medium by MTT assay	[PMID: 34982568]
MIA PaCa-2	GI₅₀	0.6 μM Compound: 1	Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for overnight in glucose-containing medium followed by compound addition and measured after 7 days by MTT assay Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for overnight in glucose-containing medium followed by compound addition and measured after 7 days by MTT assay	[PMID: 35167303]
MIA PaCa-2	IC₅₀	118.5 nM Compound: 2; DX2-201	Inhibition of oxidative phosphorylation in human MIA PaCa-2 cells assessed as reduction in ATP production incubated for 24 hrs in galactose-containing medium by CellTiter-glo luminescence assay Inhibition of oxidative phosphorylation in human MIA PaCa-2 cells assessed as reduction in ATP production incubated for 24 hrs in galactose-containing medium by CellTiter-glo luminescence assay	[PMID: 34982568]

In Vitro

DX2-201 (cmpound 2) potently inhibits the mitochondrial function by depleting ATP production in MIA PaCa-2 cells when glucose is replaced by galactose in the medium, a condition that forces mammalian cells to rely on OXPHOS^[1].
DX2-201 depletes ATP production with an IC₅₀ value of 118.5 nM in the galactose-containing medium^[1].
DX2-201 significantly inhibits OXPHOS complex I as determined by its inhibition of oxidation of NADH to NAD+ in the NAD/NADH assay (IC₅₀ = 312 nM)^[1].
DX2-201 inhibits MIA PaCa-2 and BxPC-3 cells growth with IC₅₀ values of 0.4 μM and 0.6 μM, respectively^[1].

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

Molecular Weight

432.55

Formula

C₁₈H₂₈N₂O₆S₂

CAS No.

2749554-00-3

SMILES

O=S(N1C[C@@H](CCC1)C(OCC)=O)(C2=CC=C(C=C2)S(N(CC)CC)(=O)=O)=O

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]. Ding Xue, et al. Discovery and Lead Optimization of Benzene-1,4-disulfonamides as Oxidative Phosphorylation Inhibitors.J Med Chem. 2022 Jan 13;65(1):343-368. https://pubmed.ncbi.nlm.nih.gov/34982568/

DX2-201 Related Classifications

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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:

DX2-2012749554-00-3Oxidative PhosphorylationMitochondrial MetabolismOXPHOS complex I inhibitoranticancer effectsmitochondrial functionATP productionInhibitorinhibitorinhibit

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