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Cat. No.: HY-W167448

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DHFR-IN-28

DHFR-IN-28 is an inhibitor of Plasmodium falciparum dihydrofolate reductase (DHFR), with a K_i value of 20.0 nM against wild-type pfDHFR. DHFR-IN-28 inhibits the growth of both wild-type and A16V+S108T mutant Plasmodium falciparum. DHFR-IN-28 is applicable for research related to malaria.

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

CAS No.: 1931-17-5
Formula: C₁₁H₁₆ClN₅
Molecular Weight:253.73

Storage:

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

DHFR-IN-28 Chemical Structure

CAS No.: 1931-17-5

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Use of MCE Products

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

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

Description

IC₅₀ & Target^[1]

Plasmodium

All Parasite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	GI₅₀	6.6 μM Compound: T1	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 26994844]
Huh-7	CC₅₀	>83.66 μM Compound: GNF-Pf-3611	NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7) NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)	[PMID: 18579783]
MCF7	GI₅₀	12.7 μM Compound: T1	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 26994844]

In Vitro

DHFR-IN-28 (compound 22) inhibits wild-type Plasmodium falciparum DHFR with a K_i of 20 nM and A16V+S108T mutant Plasmodium falciparum DHFR with a K_i of 1375 nM, showing a 69-fold difference in potency between the mutant and wild-type enzymes^[1].
DHFR-IN-28 inhibits growth of wild-type Plasmodium falciparum TM4/8.2 with an IC₅₀ of 546 nM and A16V+S108T mutant Plasmodium falciparum T9/94 RC17 with an IC₅₀ of 445 nM, showing slightly greater potency against the mutant parasite strain^[1].

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

Chemical Information

CAS No. 1931-17-5
Molecular Weight 253.73
Formula C₁₁H₁₆ClN₅
SMILES

NC1=NC(N)=NC(C)(C)N1C2=CC=CC=C2.Cl
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]. Yuthavong Y, et al. Development of a lead inhibitor for the A16V+S108T mutant of dihydrofolate reductase from the cycloguanil-resistant strain (T9/94) of Plasmodium falciparum. Journal of medicinal chemistry. 2000 Jul 13;43(14):2738-44. [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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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DHFR-IN-28

All Parasite Isoforms