PMMB276
Based on 1 Customer Validation
PMMB276, a Shikonin (HY-N0822) derivative, is a potent Tubb3 inhibitor. PMMB276 inhibits microtubule polymerization, induces G2/M cell cycle arrest and apoptosis in TNBC cells through the Cdc20/AKT2/Bcl-2 signaling axis. PMMB276 suppresses MDA-MB-231 tumor growth in mice without causing significant toxicity. PMMB276 can be used for the study of triple-negative breast cancer (TNBC).
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- CAS No.: 2209036-28-0
- Formule: C31H34O6S2
- Masse moléculaire:566.73
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L02 | IC50 |
116.2 μM
Compound: 1c
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Antiproliferative activity against human LO2 cells after 24 hrs by MTT assay.
Antiproliferative activity against human LO2 cells after 24 hrs by MTT assay.
|
29268130 |
| A549 | IC50 |
16.37 μM
Compound: 1c
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Antiproliferative activity against human A549 cells after 24 hrs by MTT assay.
Antiproliferative activity against human A549 cells after 24 hrs by MTT assay.
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29268130 |
| MDA-MB-453 | IC50 |
6.87 μM
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Inhibits the proliferation of MDA-MB-453 cells.
Inhibits the proliferation of MDA-MB-453 cells.
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38377719 |
| HepG2 | IC50 |
5.37 μM
Compound: 1c
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Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay.
Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay.
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29268130 |
| MDA-MB-231 | IC50 |
3.10 μM
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Inhibits the proliferation of MDA-MB-231 cells.
Inhibits the proliferation of MDA-MB-231 cells.
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38377719 |
| HCC1937 | IC50 |
8.92 μM
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Inhibits the proliferation of HCC1937 cells.
Inhibits the proliferation of HCC1937 cells.
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38377719 |
| MDA-MB-468 | IC50 |
4.35 μM
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Inhibits the proliferation of MDA-MB-468 cells.
Inhibits the proliferation of MDA-MB-468 cells.
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38377719 |
| MCF-10A | IC50 |
79.94 μM
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Inhibits the proliferation of MCF-10A cells.
Inhibits the proliferation of MCF-10A cells.
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38377719 |
| MDA-MB-231 | IC50 |
17.67 μM
Compound: 1c
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Antiproliferative activity against human MDA231 cells after 24 hrs by MTT assay.
Antiproliferative activity against human MDA231 cells after 24 hrs by MTT assay.
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29268130 |
| L02 | IC50 |
69.46 μM
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Inhibits the proliferation of L02 cells.
Inhibits the proliferation of L02 cells.
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38377719 |
| HEK-293T | IC50 |
88.83 μM
Compound: 1c
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Antiproliferative activity against human 293T cells after 24 hrs by MTT assay.
Antiproliferative activity against human 293T cells after 24 hrs by MTT assay.
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29268130 |
| HeLa | IC50 |
3.14 μM
Compound: 1c
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Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay.
Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay.
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29268130 |
PMMB276 (1-106 nM; 24 h) inhibits the proliferation of TNBC cell lines MDA-MB-231, MDA-MB-453, MDA-MB-468, and HCC1937 with IC50 values ranging from approximately 10 to 40 nM, and exhibits no significant inhibitory effects on non-cancerous MCF-10A cells at concentrations up to 100 μM[1].
PMMB276 (0.1-100 μM; 24 h) exhibits selective cytotoxicity against a panel of TNBC cell lines[1].
PMMB276 (1-8 μM; 24 h) induces apoptosis in a dose-dependent manner in MDA-MB-231 cells[1].
PMMB276 (1, 2, 4 μM; 24 h) increases cleaved caspase-3 and cleaved PARP expression, decreases total AKT2, phospho-AKT2 (Ser474), Bcl-2, and phospho-Bcl-2 (Ser70) levels, and downregulates cell cycle-associated proteins Cdc20, CDK1, and cyclin B1 in MDA-MB-231 cells[1].
PMMB276 (2, 4 μM; 24 h) induces G2/M phase cell cycle arrest in MDA-MB-231 cells, increases the proportion of cells in G2/M phase from 18.6% (control) to 43.2% (4 μM)[1].
PMMB276 (5 μM; 60 min) inhibits tubulin polymerization in vitro[1].
PMMB276-biotin (4 μM; 24 h) binds directly to Tubb3 in MDA-MB-231 cells[1].
PMMB276 (2, 4, 8 μM; 24 h) decreases Tubb3 protein expression in MDA-MB-231 cells and shows no significant effects on Tbb1 or Tubb2b expression[1].
PMMB276-biotin (4 μM; 24 h) co-localizes with Tubb3 in the cytoplasm of MDA-MB-231 cells[1].
PMMB276 (4 μM; 24 h) does not further increase apoptosis in Tubb3-knockdown MDA-MB-231 cells compared to knockdown alone[1].
PMMB276 (4 μM; 24 h) suppresses AKT2 activity in G2/M phase-synchronized cells and triggers further AKT2 downregulation upon Cdc20 knockdown[1].
PMMB276 (4 μM; 24 h) increases the expression of pro-apoptotic genes Bad, Bax, and PARP in MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, MCF-10A, L-02
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Concentration:0.1, 1, 10, 100 μM
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Incubation Time:24 h
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Result:Inhibited MDA-MB-231 cell proliferation with an IC50 of 3.10 μM.
Showed no inhibitory effects on non-cancer cell lines MCF-10A and L-02 at concentrations up to 100 μM.
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Cell Line:TNBC cell lines (MDA-MB-231, MDA-MB-453, MDA-MB-468, HCC1937, BT474) and MCF-10A
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Concentration:1-10[6] nM
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Incubation Time:24 h
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Result:Showed selective cytotoxicity against TNBC cells.
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Cell Line:MDA-MB-231 cells
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Concentration:1, 2, 4, 8 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner.
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Cell Line:MDA-MB-231 cells
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Concentration:2, 4 μM
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Incubation Time:24 h
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Result:Induced G2/M phase cell cycle arrest.
Increased the proportion of cells in G2/M phase from 18.6% to 43.2% (4 μM).
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Cell Line:MDA-MB-231 cells
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Concentration:1, 2, 4 μM
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Incubation Time:24 h
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Result:Increased cleaved caspase-3 and cleaved PARP.
Decreased total AKT2, p-AKT2 (Ser474), Bcl-2, p-Bcl-2 (Ser70).
Downregulated Cdc20, CDK1, and cyclin B1 expression.
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Cell Line:MDA-MB-231 cells
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Concentration:2, 4, 8 μM
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Incubation Time:24 h
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Result:Decreased Tubb3 protein expression; no effect on Tbb1 or Tubb2b.
Showed no significant effects on Tbb1 or Tubb2b expression.
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Cell Line:MDA-MB-231 cells (siCdc20)
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Concentration:4 μM
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Incubation Time:24 h
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Result:Triggered further AKT2 downregulation.
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Cell Line:MDA-MB-231 cells
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Concentration:4 μM
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Incubation Time:24 h
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Result:Co-localized with Tubb3 in the cytoplasm.
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Cell Line:MDA-MB-231 cells (siTubb3 or PMMB276-treated)
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Concentration:4 μM
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Incubation Time:24 h
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Result:Increased expression of pro-apoptotic genes Bad, Bax, and PARP.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA-MB-231 xenograft model in female Balb/c nude mice (4-5 weeks old, 18-20 g)[1]
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Dosage:2, 4 mg/kg
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Administration:i.p.; every other day for 14 days
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Result:Suppressed tumor growth vs vehicle.
Reduced tumor weight-to-body weight ratio.
Showed no significant body weight change.
Showed no obvious toxicity.
Decreased Ki-67 expression in tumor tissues.
Prolonged overall survival.
Decreased Tubb3 and AKT2 expression in tumors.
Chemical Information
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CAS No. 2209036-28-0
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Appearance Solid
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Masse moléculaire 566.73
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Formule C31H34O6S2
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Color Brown to reddish brown
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SMILES
O=C(C1=C(C=CC(O)=C12)O)C=C([C@@H](C/C=C(C)/C)OC(CCCC[C@H]3SC(SCC3)C4=CC=CC=C4)=O)C2=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Pureté et documentation
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Fiche technique (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PMMB276 Related Classifications
HY-158208 Related Classifications
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