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PCLX-001

Catalog No. T63788 CAS 1215011-08-7

PCLX-001 is a small-molecule compound that acts as an orally active inhibitor of N-myristoyltransferase (NMT), specifically targeting NMT1 and NMT2 with IC50 values of 5 nM and 8 nM, respectively. This compound demonstrates anti-tumor effects and effectively inhibits the early signaling of B-cell receptor (BCR). Consequently, PCLX-001 is a valuable tool for researching B-cell malignancies [1] [2].

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PCLX-001, CAS 1215011-08-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 229.00
5 mg	In stock	$ 578.00
10 mg	In stock	$ 833.00
25 mg	In stock	$ 1,270.00
50 mg	In stock	$ 1,690.00
100 mg	In stock	$ 2,290.00
500 mg	In stock	$ 4,620.00
1 mL * 10 mM (in DMSO)	In stock	$ 733.00

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Biological Description

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Description	PCLX-001 is a small-molecule compound that acts as an orally active inhibitor of N-myristoyltransferase (NMT), specifically targeting NMT1 and NMT2 with IC50 values of 5 nM and 8 nM, respectively. This compound demonstrates anti-tumor effects and effectively inhibits the early signaling of B-cell receptor (BCR). Consequently, PCLX-001 is a valuable tool for researching B-cell malignancies [1] [2].
Targets&IC50	NMT2:8 nM, NMT1:5 nM
In vitro	We discovered a marked sensitivity of hematological cancer cell lines, including B-cell lymphomas, to the potent pan-NMT inhibitor PCLX-001. PCLX-001 treatment impacts the global myristoylation of lymphoma cell proteins and inhibits early B-cell receptor (BCR) signaling events critical for survival. In addition to abrogating myristoylation of Src family kinases, PCLX-001 also promotes their degradation and, unexpectedly, that of numerous non-myristoylated BCR effectors including c-Myc, NFκB and P-ERK, leading to cancer cell death in vitro and in xenograft models.[2]
In vivo	Treatment of cultured breast cancer cells with PCLX-001 reduced cell viability in vitro. Daily oral administration of PCLX-001 to immunodeficient mice bearing human MDA-MB-231 breast cancer xenografts produced significant dose-dependent tumor growth inhibition in vivo.[4]

Molecular Weight	537.51
Formula	C24H30Cl2N6O2S
CAS No.	1215011-08-7

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.38 mg/mL (10 mM)

References and Literature

1. Weickert M, et al. Initial characterization and toxicology of an nmt inhibitor in development for hematologic malignancies. Blood. 2019;134: 3362. 2. Beauchamp E, et al. Targeting N-myristoylation for therapy of B-cell lymphomas. Nat Commun. 2020;11(1):5348. 3. Sangha R, et al. Novel, First-in-Human, Oral PCLX-001 Treatment in a Patient with Relapsed Diffuse Large B-Cell Lymphoma. Curr Oncol. 2022;29(3):1939-1946. 4. Mackey JR, et al. N-myristoyltransferase proteins in breast cancer: prognostic relevance and validation as a new drug target. Breast Cancer Res Treat. 2021;186(1):79-87.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library Clinical Compound Library Anti-Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PCLX-001 1215011-08-7 Others inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.