2. Epigenetics
  3. Histone Acetyltransferase
  4. PU141

PU141 

Cat. No.: HY-120290
Handling Instructions

PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity.

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

PU141 Chemical Structure

PU141 Chemical Structure

CAS No. : 168334-34-7

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Description

PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity[1].

IC50 & Target

CBP/p300[1]
In Vitro

PU141 inhibits cell growth at micromolar concentrations in A431 (epidemoid carcinoma), A549 (alveolar basal epithelial adenocarcinoma), A2780 (ovarian carcinoma), HCT116 (epithelial colon carcinoma), HepG2 (hepatocellular carcinoma), MCF7 (breast carcinoma), SK-N-SH (neuroblastoma), SW480 (colon adenocarcinoma) and U-87MG (epithelial-like glioblastoma-astrocytoma)[1].
PU141 causes both histone hypoacetylation and growth inhibition in vitro. PU141 (25 µM) leads to a decrease in SAHA-induced H3K14 and H4K8 hyperacetylation, whereas H3K9 and H4K16 acetylation levels remaine stable after co-treatment of HDAC and HAT inhibitor. The impact on histone acetylation is similar in both SK-N-SH and HCT116 cells[1].

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

Cell Viability Assay[1]

Cell Line: A431 (epidemoid carcinoma), A549 (alveolar basal epithelial adenocarcinoma), A2780 (ovarian carcinoma), HCT116 (epithelial colon carcinoma), HepG2 (hepatocellular carcinoma), MCF7 (breast carcinoma), SK-N-SH (neuroblastoma), SW480 (colon adenocarcinoma) and U-87MG (epithelial-like glioblastoma-astrocytoma)
Concentration: 0, 10, 20, 30, 40, 50, and 60 µM
Incubation Time:
Result: Inhibited cell growth at micromolar concentrations in all screened cell lines. The highest cellular antiproliferative activity was detected for the neuroblastoma SK-N-SH cell line.

Western Blot Analysis[1]

Cell Line: SK-N-SH neuroblastoma and HCT116 colon carcinoma cells
Concentration: 25 µM
Incubation Time: 3 hours
Result: Led to a decrease in SAHA-induced H3K14 and H4K8 hyperacetylation.
In Vivo

PU141 (25 mg/kg; administered once intraperitoneally for 24 days) exhibits a significant antitumor effects against neuroblastoma xenografts in vivo[1].

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

Animal Model: Male NMRI:nu/nu mice bearing a xenograft model[1]
Dosage: 12.5 and 25 mg/kg
Administration: Administered once intraperitoneally (i.p.) as a detergent containing saline microemulsion; for 24 days
Result: Led to significant tumor volume reduction (19%) at 25 mg/kg.
Molecular Weight

310.29

Formula

C14H9F3N2OS
CAS No.
SMILES

O=C1N(SC2=NC=CC=C21)CC3=CC=C(C=C3)C(F)(F)F
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
References
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Help & FAQs
  • 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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Keywords:

PU141168334-34-7PU 141PU-141Histone AcetyltransferaseHATsHATp300 HATCBP/p300 selectivityKAT3-selective inhibitorpyridoisothiazoloneanticancerInhibitorinhibitorinhibit

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