1. Apoptosis
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  3. Pladienolide B

Pladienolide B 

Cat. No.: HY-16399
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Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis.

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Pladienolide B Chemical Structure

Pladienolide B Chemical Structure

CAS No. : 445493-23-2

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Description

Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis[1][2][3].

In Vitro

Pladienolide B (0.1-2 nM; 24-72 hours) inhibits human cervical carcinoma cells viability[3].
Pladienolide B (0.1-2 nM; 24-48 hours) reduces SF3b1 expression in human cervical carcinoma cells[3].
Pladienolide B induces (0.1-2 nM; 24 hours) cell cycle arrest and apoptosis[3].

Cell Viability Assay[3]

Cell Line: HeLa cells
Concentration: 0.1, 0.5, 1, 1.5, 2 nM
Incubation Time: 24, 48, 72 hours
Result: Significantly decreased cell viability, and the decrease was concentration- and time-dependent.

Apoptosis Analysis[3]

Cell Line: HeLa cells
Concentration: 0.1, 0.5, and 2 nM
Incubation Time: 24 hours
Result: The apoptotic cells were highly induced at 24 hours.

RT-PCR[3]

Cell Line: HeLa cells
Concentration: 0.1, 0.5, and 2 nM
Incubation Time: 24, 48 hours
Result: Induced a time- and concentration-dependent decrease in cellular SF3b1 proteins.
In Vivo

Pladienolide B (2.5-10 mg/kg; i.v.; daily for 5 days) has strong antitumor activities[4].

Animal Model: Female or male BALB/c nu/nu mice (7 weeks of age) (PC-3, OVCAR-3, DU-145, WiDr, and HCT-116, BSY-1 xenografts)[4]
Dosage: 2.5, 5, and 10 mg/kg
Administration: I.v.; daily for 5 days
Result: Showed strong growth inhibitory or regressive activities against these xenografts.
Molecular Weight

536.70

Formula

C₃₀H₄₈O₈

CAS No.

445493-23-2

SMILES
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Keywords:

Pladienolide BApoptosismacrolideantitumorpre-mRNAsplicingcervicalcarcinomaHeLacellsSF3b1cyclearrestInhibitorinhibitorinhibit

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Pladienolide B
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HY-16399
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