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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.

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

CAS No.: 2749554-00-3
Formula: C₁₈H₂₈N₂O₆S₂
Molecular Weight:432.55

Storage:

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

Data Sheet (267 KB)

DX2-201 Chemical Structure

CAS No.: 2749554-00-3

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

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	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	>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	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.

Chemical Information

CAS No. 2749554-00-3
Molecular Weight 432.55
Formula C₁₈H₂₈N₂O₆S₂
SMILES

O=S(N1C[C@@H](CCC1)C(OCC)=O)(C2=CC=C(C=C2)S(N(CC)CC)(=O)=O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (1)

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2025 Apr 11.

Purity & Documentation

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Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 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]. 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/

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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
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (1)
Purity & Documentation
References

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