2. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  3. DNA/RNA Synthesis ADC Cytotoxin
  4. α-Amanitin

α-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.

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

α-Amanitin Chemical Structure

α-Amanitin Chemical Structure

CAS No. : 23109-05-9

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Customer Review

Based on 37 publication(s) in Google Scholar

Other Forms of α-Amanitin:

α-Amanitin Related Antibodies

Top Publications Citing Use of Products

37 Publications Citing Use of MCE α-Amanitin

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Description

α-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.

IC50 & Target

Traditional Cytotoxic Agents

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
1 μM
Compound: Alpha-amanitin
Cytotoxicity against chinese hamster CHO cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against chinese hamster CHO cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 35696491]
HEK293 IC50
1 μM
Compound: Alpha-amanitin
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 35696491]
HeLa IC50
1 μM
Compound: Alpha-amanitin
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 35696491]
HepG2 IC50
0.56 μM
Compound: Alpha-amanitin
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 35696491]
In Vitro

α-Amanitin decreases TAF15 mRNA and TAF15 protein levels in MKN45 cells, and inhibits the RNAPII activity towards TAF15 mRNA[2]. alpha-Amanitin decreases cell viability by 14%, 21%, 41%, 44%, and 50% at concentrations of 100, 10, 1, 0.1, and 0.01 μg/mL, respectively. The LD50 of the alpha-Amanitin at 36 h is measured as 1 μg/mL. The total amount of protein within the cell at 24 h is significantly increased for the 1 μg/mL dose of alpha-Amanitin compared to the control[3]. α-Amanitin dramatically decreases the expression of gap junctional genes (Gja1, Gja4 and Gjc1) and FSHr and LHr in cumulus cells[4].

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

α-Amanitin Related Antibodies
In Vivo

The intravenous LD50 dose of alpha-Amanitin is 0.327 mg/kg body weight after intravenous injection into BALB/c mice. After 12 h of alpha-Amanitin injection in caudal vein, the levels of WBC, RBC and HGB decrease significantly, while those of BUN and Crea increase significantly in serum. alpha-Amanitin inhibits some genes (Hsp90b1, Irx4, etc.), whose encoded proteins regulate the RNA polymerase II activity. alpha-Amanitin down-regulates some proteins (Nmi, Trpc5, etc.) taking part in the transcription progress[1]. alpha-Amanitin has potent activity in DTC suppression. Mice injected with alpha-Amanitin (0.4 mg/kg, i.p.)-treated cells maintain their body weight, while those receiving a peritoneal injection of MKN45 cells show a constant decrease in body weight[2].

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

918.97

Formula

C39H54N10O14S
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=[S@](C[C@@](NC(CNC([C@@]([C@@H](C)CC)([H])N1)=O)=O)([H])C(N[C@@](C(N(C[C@H](O)C2)[C@]2([H])C3=O)=O)([H])CC(N)=O)=O)C4=C(C[C@](C(NCC1=O)=O)([H])NC([C@](N3)([H])[C@@H](C)[C@@H](O)CO)=O)C5=CC=C(O)C=C5N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (108.82 mM; Need ultrasonic)

DMSO : 100 mg/mL (108.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0882 mL 5.4409 mL 10.8817 mL
5 mM 0.2176 mL 1.0882 mL 2.1763 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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: ≥ 2.5 mg/mL (2.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (2.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 25 mg/mL (27.20 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.92%

SDS (584 KB)

COA (256 KB) HNMR (317 KB) LCMS (261 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[3]

The MTT assay is used to evaluate the overall functional integrity and viability of the cultured cells. The MCF-7 cells are put into 96-well plates (2×104 for each well), which are incubated for 24 h. The specific concentrations of alpha-Amanitin and β-Amanitin are added to the cell culture medium, and plates are incubated for an additional 36 h. MTT solution (1:10 ratio) and dimethyl sulfoxide (DMSO) (100 µL) are then added to the cell culture medium and plates are incubated overnight. The absorbance is measured at 570 nm on a plate reader. This experiment is repeated 3 times. The absorbance data are calculated as percentages according to the control group.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

For tumorigenicity tests, six colonies (untreated) and DTCs derived from MKN45 cells are individually injected subcutaneously into the left and right side of the backs of six 6-week-old female nude mice (BALB/cAjcl-nu/nu). These mice are monitored for 49 days after the inoculation or until tumors reach 10 mm in the largest diameter, and are then euthanized. For the PC model, 1.0×106 MKN45 cells are injected intraperitoneally into six 6-week-old female nude mice (BALB/cAjcl-nu/nu). Mice are then treated with CIS (4.0 mg/kg, intraperitoneal administration) or a combination of CIS and alpha-Amanitin (0.4 mg/kg, intraperitoneal administration). For the combination treatment, alpha-Amanitin is given 24 hours before CIS. Body weight is monitored for 28 days after the treatment.

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.0882 mL 5.4409 mL 10.8817 mL 27.2044 mL
5 mM 0.2176 mL 1.0882 mL 2.1763 mL 5.4409 mL
10 mM 0.1088 mL 0.5441 mL 1.0882 mL 2.7204 mL
15 mM 0.0725 mL 0.3627 mL 0.7254 mL 1.8136 mL
20 mM 0.0544 mL 0.2720 mL 0.5441 mL 1.3602 mL
25 mM 0.0435 mL 0.2176 mL 0.4353 mL 1.0882 mL
30 mM 0.0363 mL 0.1814 mL 0.3627 mL 0.9068 mL
40 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6801 mL
50 mM 0.0218 mL 0.1088 mL 0.2176 mL 0.5441 mL
60 mM 0.0181 mL 0.0907 mL 0.1814 mL 0.4534 mL
80 mM 0.0136 mL 0.0680 mL 0.1360 mL 0.3401 mL
100 mM 0.0109 mL 0.0544 mL 0.1088 mL 0.2720 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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α-Amanitin Related Classifications

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.

Keywords:

α-Amanitin23109-05-9α-AmatoxinDNA/RNA SynthesisADC CytotoxinADC PayloadInhibitorinhibitorinhibit

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