Art. -Nr.: HY-158208

PMMB276

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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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Reinheit: 99.81%
CAS. Nr.: 2209036-28-0
Formel: C₃₁H₃₄O₆S₂
Molecular Weight:566.73

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PMMB276 Chemical Structure

CAS. Nr.: 2209036-28-0

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC50	3.10 μM	Antiproliferative activity against human MDA-MB-231 TNBC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MDA-MB-231 TNBC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay	38377719
MDA-MB-468	IC50	4.35 μM	Antiproliferative activity against human MDA-MB-468 TNBC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MDA-MB-468 TNBC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay	38377719
MDA-MB-453	IC50	6.87 μM	Antiproliferative activity against human MDA-MB-453 TNBC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MDA-MB-453 TNBC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay	38377719
HCC1937	IC50	8.92 μM	Antiproliferative activity against human HCC1937 TNBC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCC1937 TNBC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay	38377719
MCF-10A	IC50	79.94 μM	Cytotoxicity against human MCF-10A mammary epithelial cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay Cytotoxicity against human MCF-10A mammary epithelial cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay	38377719
L02	IC50	69.46 μM	Cytotoxicity against human L-02 normal hepatocytes assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay Cytotoxicity against human L-02 normal hepatocytes assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo Luminescent Cell Viability Assay	38377719

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:

MDA-MB-231, MCF-10A, L-02
Concentration:

0.1, 1, 10, 100 μM
Incubation Time:

24 h
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.

Cell Viability Assay^[1]

Cell Line:

TNBC cell lines (MDA-MB-231, MDA-MB-453, MDA-MB-468, HCC1937, BT474) and MCF-10A
Concentration:

1-10^[6] nM
Incubation Time:

24 h
Result:

Showed selective cytotoxicity against TNBC cells.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

1, 2, 4, 8 μM
Incubation Time:

24 h
Result:

Induced apoptosis in a dose-dependent manner.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

2, 4 μM
Incubation Time:

24 h
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).

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

1, 2, 4 μM
Incubation Time:

24 h
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.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

2, 4, 8 μM
Incubation Time:

24 h
Result:

Decreased Tubb3 protein expression; no effect on Tbb1 or Tubb2b.
Showed no significant effects on Tbb1 or Tubb2b expression.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 cells (siCdc20)
Concentration:

4 μM
Incubation Time:

24 h
Result:

Triggered further AKT2 downregulation.

Immunofluorescence^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

4 μM
Incubation Time:

24 h
Result:

Co-localized with Tubb3 in the cytoplasm.

RT-PCR^[1]

Cell Line:

MDA-MB-231 cells (siTubb3 or PMMB276-treated)
Concentration:

4 μM
Incubation Time:

24 h
Result:

Increased expression of pro-apoptotic genes Bad, Bax, and PARP.

In Vivo

PMMB276 (2 and 4 mg/kg; i.p.; every other day for 14 days) in female Balb/c nude mice bearing MDA-MB-231 xenografts significantly suppresses tumor growth, reduces tumor weight-to-body weight ratio, does not significantly alter body weight, decreases Ki-67 expression in tumor tissues, prolongs overall survival, and decreases Tubb3 and AKT2 protein expression in tumor tissues^[1].

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

Animal Model:

MDA-MB-231 xenograft model in female Balb/c nude mice (4-5 weeks old, 18-20 g)^[1]
Dosage:

2, 4 mg/kg
Administration:

i.p.; every other day for 14 days
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

CAS. Nr. 2209036-28-0
Appearance Solid
Molecular Weight 566.73
Formel C₃₁H₃₄O₆S₂
Color Brown to reddish brown
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (176.45 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7645 mL

8.8225 mL

17.6451 mL

5 mM

0.3529 mL

1.7645 mL

3.5290 mL

10 mM

0.1765 mL

0.8823 mL

1.7645 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (8.82 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (8.82 mM); Suspended solution

This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (8.82 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Han H, et al. A modified natural small molecule inhibits triple-negative breast cancer growth by interacting with Tubb3. Phytomedicine. 2024 Apr;126:154894. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7645 mL	8.8225 mL	17.6451 mL	44.1127 mL
	5 mM	0.3529 mL	1.7645 mL	3.5290 mL	8.8225 mL
	10 mM	0.1765 mL	0.8823 mL	1.7645 mL	4.4113 mL
	15 mM	0.1176 mL	0.5882 mL	1.1763 mL	2.9408 mL
	20 mM	0.0882 mL	0.4411 mL	0.8823 mL	2.2056 mL
	25 mM	0.0706 mL	0.3529 mL	0.7058 mL	1.7645 mL
	30 mM	0.0588 mL	0.2941 mL	0.5882 mL	1.4704 mL
	40 mM	0.0441 mL	0.2206 mL	0.4411 mL	1.1028 mL
	50 mM	0.0353 mL	0.1765 mL	0.3529 mL	0.8823 mL
	60 mM	0.0294 mL	0.1470 mL	0.2941 mL	0.7352 mL
	80 mM	0.0221 mL	0.1103 mL	0.2206 mL	0.5514 mL
	100 mM	0.0176 mL	0.0882 mL	0.1765 mL	0.4411 mL

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PMMB276

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PMMB276 Related Classifications

HY-158208 Related Classifications

Bioz