1. PROTAC Anti-infection Metabolic Enzyme/Protease
  2. PROTACs Parasite Dihydrofolate reductase (DHFR)
  3. BION106

BION106 is a dihydrofolate reductasethymidylate synthase (DHFR-TS) PROTAC degrader. BION106 exhibits extremely strong anti-malarial activity with a Ki and toxicity of 2.68 nM and 0.2 μM against Plasmodium falciparum, and > 100 μM and 44.2 μM in mammalian cells. BION106 can be used for the study of antimalarial parasites (Blue: Idasanutlin ligand (HY-15676); Pink: DHFR-TS ligand (HY-153007); Black: Linker (HY-W021401)).

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

BION106

BION106 Chemical Structure

CAS No. : 3077918-44-3

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Description

BION106 is a dihydrofolate reductasethymidylate synthase (DHFR-TS) PROTAC degrader. BION106 exhibits extremely strong anti-malarial activity with a Ki and toxicity of 2.68 nM and 0.2 μM against Plasmodium falciparum, and > 100 μM and 44.2 μM in mammalian cells. BION106 can be used for the study of antimalarial parasites (Blue: Idasanutlin ligand (HY-15676); Pink: DHFR-TS ligand (HY-153007); Black: Linker (HY-W021401))[1].

In Vitro

BION106 (10 μM, 30-240 min) rapidly and efficiently degrades the dihydrofolate reductase-thymidylate synthase, which indicates that it can quickly form a productive ternary complex and initiate the degradation processPlasmodium falciparum[1].
BION106 (0.4-50 μM, 4 h) significantly reduces the content of dihydrofolate reductase-thymidylate synthase in the Plasmodium falciparum in a concentration-dependent manner[1].

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

Molecular Weight

1133.12

Formula

C57H69Cl2F2N9O9

CAS No.
SMILES

N#C[C@@]1(C2=C(C=C(C=C2)Cl)F)[C@@H](C3=C(C(Cl)=CC=C3)F)[C@@H](N[C@H]1CC(C)(C)C)C(NC4=C(C=C(C=C4)C(NCCOCCOCCOCCNC(CCC5=C(C=CC=C5)OCCCOC6=C(N)N=C(N)N=C6CC)=O)=O)OC)=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.

Purity & Documentation
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  • 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.

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BION106
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HY-178728
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