Art. -Nr.: HY-119376

MDL-800

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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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Reinheit: 99.11%
CAS. Nr.: 2275619-53-7
Formel: C₂₁H₁₆BrCl₂FN₂O₆S₂
Molecular Weight:626.30

Speicherung:

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

MDL-800 Chemical Structure

CAS. Nr.: 2275619-53-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle Sirtuin Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
ASPC1	IC₅₀	50.51 μM Compound: MDL-800	Antiproliferative activity against human AsPC1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human AsPC1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32787077]
Bel-7402	IC₅₀	18.6 μM Compound: 7a; MDL-800	Antiproliferative activity against human Bel-7402 cells Antiproliferative activity against human Bel-7402 cells	[PMID: 34213345]
BXPC-3	IC₅₀	57.96 μM Compound: MDL-800	Antiproliferative activity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32787077]
MIA PaCa-2	IC₅₀	55.65 μM Compound: MDL-800	Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32787077]
PANC-1	IC₅₀	35.19 μM Compound: MDL-800	Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32787077]
PLC-PRF-5	IC₅₀	18.6 μM Compound: 7a; MDL-800	Antiproliferative activity against human PLCPRF5 cells Antiproliferative activity against human PLCPRF5 cells	[PMID: 34213345]

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.

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.

Chemical Information

CAS. Nr. 2275619-53-7
Appearance Solid
Molecular Weight 626.30
Formel C₂₁H₁₆BrCl₂FN₂O₆S₂
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
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

Publications (2)

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Journal Impact Factor

Biochem Pharmacol

SIRT6 activation attenuates inflammatory-fibrogenic events, improves lung function and survival in experimental pulmonary fibrosis. [Abstract]

2026 Aug;250(Pt 1):117940. PMID: 41916469
Aging Med (Milton)

Visualization of OPN-Targeted Self-Assembled Micelles Encapsulated With an SIRT6 Activator and Doped Indocyanine Green for Attenuating Vascular Aging. [Abstract]

2025 Oct 26;8(5):383-397. PMID: 41180385

Lösungsmittel & Löslichkeit

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)

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

1.5967 mL

7.9834 mL

15.9668 mL

5 mM

0.3193 mL

1.5967 mL

3.1934 mL

10 mM

0.1597 mL

0.7983 mL

1.5967 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: ≥ 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.

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 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 (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Huang Z, et al. Identification of a cellularly active SIRT6 allosteric activator. Nat Chem Biol. 2018 Dec;14(12):1118-1126. [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	1.5967 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

Keywords

MDL-800

2 Cited Publications

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MDL-800

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Glutamine Metabolism Compound Library

Targeted Diversity Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MDL-800

Alle Sirtuin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MDL-800

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Glutamine Metabolism Compound Library

Targeted Diversity Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MDL-800

Alle Sirtuin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MDL-800 Related Classifications

HY-119376 Related Classifications