2. Cell Cycle/DNA Damage Epigenetics
  3. Sirtuin
  4. MDL-800

MDL-800 is an allosteric and selective SIRT6 activator. MDL-800 increases SIRT6 deacetylation activity with an EC50 of 10.3 µM.

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MDL-800

MDL-800 Chemical Structure

CAS No. : 2275619-53-7

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Based on 1 publication(s) in Google Scholar

MDL-800 Related Antibodies

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1 Publications Citing Use of MCE MDL-800

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MDL-800 is an allosteric and selective SIRT6 activator. MDL-800 increases SIRT6 deacetylation activity with an EC50 of 10.3 µM[1].

IC50 & Target[1]

SIRT6

10.3 μM (EC50)

In Vitro

MDL-800 potently activates SIRT6 at ~10 µM but shows no activity toward SIRT1, SIRT3, SIRT4, and HDAC1-11 at concentrations up to 50 or 100 µM. Although MDL-800 exhibits weak activity toward SIRT2, SIRT5, and SIRT7, the EC50 or IC50 values are greater than 100 µM, tenfold less than that against SIRT6[1].
MDL-800 directly activates SIRT6 deacetylation by increasing the binding affinities of acetylated substrates and cofactor as well as increasing the catalytic efficiency of SIRT6[1].
MDL-800 (1-1000 μM; 48 hours) decreases the proliferation of Bel7405, PLC/PRF/5, and Bel7402 cells with IC50s for cell growth (IC50-growth) of 23.3 μM, 18.6 μM, and 24.0 μM, respectively, and EC50s for cell death (EC50-death) of 90.4 μM, 87.0 μM, and 106.5 μM, respectively[1].
MDL-800 (0-50 μM; 24 and 48 hours) decreases both H3K9ac and H3K56ac at a concentration of 10 µM and shows a dose-dependent effect in Bel7405, PLC/PRF/5, and Bel7402 cells at 24 and 48 h[1].

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

MDL-800 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Bel7405, PLC/PRF/5, and Bel7402 cells
Concentration: 1, 10, 100 , 1000 μM
Incubation Time: 48 hours
Result: Decreased the proliferation of Bel7405, PLC/PRF/5, and Bel7402 cells with IC50s of 23.3 μM, 18.6 μM, and 24.0 μM, respectively.

Western Blot Analysis[1]

Cell Line: Bel7405, PLC/PRF/5, and Bel7402 cells
Concentration: 0, 5, 10, 25, and 50 μM
Incubation Time: 24 and 48 hours
Result: Decreased both H3K9ac and H3K56ac at a concentration of 10 µM and showed a dose-dependent effect in all three cell lines at 24 h and 48 h.
In Vivo

MDL800 shows effective antitumor efficacy in female BALB/c nude mice with Bel7405 xenograft tumor mode. MDL800 (50-150 mg/kg; intraperitoneal injection; over 2 weeks) suppresses the growth of Bel7405 xenografts in a dose-dependent manner compared with vehicle alone[1].

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

Animal Model: Six-week-old female BALB/c nude mice with Bel7405 xenograft tumor mode[1]
Dosage: 50, 100, and 150 mg/kg
Administration: Intraperitoneal injection; over 2 weeks.
Result: Suppressed the growth of Bel7405 xenografts in a dose-dependent manner. Decreased tumor weight and size.
Molecular Weight

626.30

Formula

C21H16BrCl2FN2O6S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(S(NC2=CC=C(S(NC3=CC(Br)=C(F)C=C3C)(=O)=O)C(C(OC)=O)=C2)(=O)=O)=CC(Cl)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (199.58 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 1.5967 mL 7.9834 mL 15.9668 mL
5 mM 0.3193 mL 1.5967 mL 3.1934 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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: ≥ 2.08 mg/mL (3.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.11%

SDS (393 KB)

COA (254 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5967 mL 7.9834 mL 15.9668 mL 39.9170 mL
5 mM 0.3193 mL 1.5967 mL 3.1934 mL 7.9834 mL
10 mM 0.1597 mL 0.7983 mL 1.5967 mL 3.9917 mL
15 mM 0.1064 mL 0.5322 mL 1.0645 mL 2.6611 mL
20 mM 0.0798 mL 0.3992 mL 0.7983 mL 1.9958 mL
25 mM 0.0639 mL 0.3193 mL 0.6387 mL 1.5967 mL
30 mM 0.0532 mL 0.2661 mL 0.5322 mL 1.3306 mL
40 mM 0.0399 mL 0.1996 mL 0.3992 mL 0.9979 mL
50 mM 0.0319 mL 0.1597 mL 0.3193 mL 0.7983 mL
60 mM 0.0266 mL 0.1331 mL 0.2661 mL 0.6653 mL
80 mM 0.0200 mL 0.0998 mL 0.1996 mL 0.4990 mL
100 mM 0.0160 mL 0.0798 mL 0.1597 mL 0.3992 mL
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MDL-800 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:

MDL-8002275619-53-7MDL800MDL 800SirtuinInhibitorinhibitorinhibit

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