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Art. -Nr.: HY-186330

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PMM-302

Name: PMM-302
Brand: MedChemExpress
SKU: HY-186330
Availability: PreOrder

(Synonyms: PMMB-302)

PMM-302 (PMMB-302) is a shikonin N-benzyl sophoridate derivative and a telomerase inhibitor. PMM-302 downregulates the telomerase core proteins DKC1 and NHP2 as well as TERT mRNA, and inhibits telomerase activity. PMM-302 induces G2/M phase cell cycle arrest and apoptosis, accompanied by downregulation of Bcl2, Bcl-XL, and FADD and upregulation of cleaved caspase-3 and cleaved caspase-9. PMM-302 can be used for lung cancer-related research.

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CAS. Nr.: 2763421-81-2
Formel: C₃₈H₄₅BrN₂O₆
Molecular Weight:705.68

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

PMM-302 Chemical Structure

CAS. Nr.: 2763421-81-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

Telomerase

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Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC50	8.05 μM	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human HeLa cells assessed as reduction in cell viability by CCK8 assay.	34922028
MDA-MB-231	IC50	4.72 μM	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by CCK8 assay.	34922028
MCF7	IC50	7.12 μM	Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability by CCK8 assay.	34922028
A549	IC50	2.71 μM	Antiproliferative activity against human A549 cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human A549 cells assessed as reduction in cell viability by CCK8 assay.	34922028
L02	IC50	93.81 μM	Cytotoxicity against non-cancerous human L0-2 cells assessed as reduction in cell viability by CCK8 assay. Cytotoxicity against non-cancerous human L0-2 cells assessed as reduction in cell viability by CCK8 assay.	34922028
Calu-3	IC50	16.02 μM	Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability by CCK8 assay.	34922028
NCI-H460	IC50	5.34 μM	Antiproliferative activity against human H460 cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human H460 cells assessed as reduction in cell viability by CCK8 assay.	34922028
NCI-H1650	IC50	5.45 μM	Antiproliferative activity against human H1650 cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human H1650 cells assessed as reduction in cell viability by CCK8 assay.	34922028

In Vitro

Anti-cancerCell Cycle RegulationApoptosisOthers

Anti-cancer

PMM-302 (PMMB-302) inhibits the proliferation of HeLa, MDA-MB-231, MCF-7, A549, Calu-3, H460, and H1650 cancer cells with IC₅₀ values of 8.05, 4.72, 7.12, 2.71, 16.02, 5.34, and 5.45 μM, respectively; its IC₅₀ against non-cancerous L0-2 cells is 93.81 μM^[1].

Cell Cycle Regulation

PMM-302 (0-8 μM; 24 h) dose-dependently induces G2/M phase cell cycle arrest in A549 cells, with the proportion of cells in G2/M phase increasing from approximately 11.30% in the control group to approximately 23.16%, 34.42%, and 44.53% at 2, 4, and 8 μM, respectively^[1].
PMM-302 (4 μM; 0-36 h) time-dependently increases the proportion of cells in G2/M phase in A549 cells, reaching 53.40% at 36 h^[1].

Apoptosis

PMM-302 (0-4 μM; 24 h) dose-dependently induces apoptosis in A549 cells, with the proportion of late apoptotic cells increasing to 39.0% at 4 μM^[1].
PMM-302 (4 μM; 0-36 h) time-dependently increases the proportion of apoptotic cells in A549 cells^[1].

Anti-cancer

Apoptosis

PMM-302 (0-8 μM) downregulates Bcl2, Bcl-XL, and FADD and upregulates cleaved caspase-3 and cleaved caspase-9 in a concentration-dependent manner in A549 cells, supporting its apoptosis-inducing effect^[1].

Apoptosis

Anti-cancer

PMM-302 (0-8 μM) downregulates the telomerase core proteins DKC1 and NHP2 as well as TERT mRNA in A549 cells, and inhibits telomerase-related activity in a dose-dependent manner, with the most pronounced downregulation of DKC1 and NHP2 at 8 μM; its telomerase inhibitory effect is weaker than that of BIBR1532 at the same concentration^[1].

Others

Molecular docking predicts that PMM-302 localizes to the telomerase active site and forms 1 hydrogen bond with THR232^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

A549
Concentration:

0, 2, 4, 8 μM (for 24 h); 4 μM (for time-dependent assay)
Incubation Time:

24 h (for dose-dependent assay); 0, 12, 24, 36 h (for time-dependent assay)
Result:

Induced G2/M phase arrest in a dose-dependent manner with percentages of cells in G2/M phase of 11.30% (control), 23.16% (2 μM), 34.42% (4 μM), and 44.53% (8 μM).
Induced G2/M phase arrest in a time-dependent manner with maximum accumulation of 53.40% cells after treatment with 4 μM for 36 h.

Apoptosis Analysis^[1]

Cell Line:

A549
Concentration:

0, 2, 4 μM (for 24 h); 4 μM (for time-dependent assay)
Incubation Time:

24 h (for dose-dependent assay); 0, 12, 24, 36 h (for time-dependent assay)
Result:

Induced apoptosis in a dose-dependent manner with percentages of cells in late apoptosis of 5.85% (control), 29.2% (2 μM), and 39.0% (4 μM).
Induced apoptosis in a time-dependent manner with maximum accumulation of 36.6% cells in late apoptosis within 24 h.

Related Protocols :

Chemical Information

CAS. Nr. 2763421-81-2
Molecular Weight 705.68
Formel C₃₈H₄₅BrN₂O₆
SMILES

C/C(C)=C\C[C@H](C(C(C1=C(O)C=CC(O)=C12)=O)=CC2=O)OC(CCC[C@@H]3[C@]4([H])[C@]5([H])[C@](CCCN5CCC4)([H])CN3CC6=C(C=CC=C6)Br)=O
Synonyms

PMMB-302
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Han H, et al. Shikonin N-benzyl matrinic acid ester derivatives as novel telomerase inhibitors with potent activity against lung cancer cell lines. Bioorganic & medicinal chemistry letters. 2022 Feb 01;57:128503. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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PMM-302

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