PCLX-001

SKU: orb1686248

Description

PCLX-001 is a potent, orally bioavailable dual inhibitor of N-myristoyltransferases NMT1 and NMT2. It demonstrates anti-tumor activity by suppressing B-cell receptor signaling, making it a valuable research tool for studying B-cell malignancies in both in vitro and in vivo models.

Key Properties

• CAS Number: 1215011-08-7
• MW: 537.51
• Purity: 99.60% (May vary between batches)
• Formula: C₂₄H₃₀Cl₂N₆O₂S
• SMILES: N(S(=O)(=O)C1=C(Cl)C=C(C=C1Cl)C=2C=C(N=CC2)N3CCNCC3)C=4C(CC(C)C)=NN(C)C4C
• Target: Others
• Solubility: DMSO:5.38 mg/mL (10.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.86 mM)

Bioactivity

• Target IC50:
  NMT1:5 nM|NMT2:8 nM
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

N-myristoyltransferase-1 (NMT-1), NMT2

Compound Identifiers

PubChem CID

58561243