Art. -Nr.: HY-10949

SMER3

Name: SMER3
Brand: MedChemExpress
SKU: HY-10949
Price: 66.00 USD
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SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF)^Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCF^Met30.

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Reinheit: 98.33%
CAS. Nr.: 67200-34-4
Formel: C₁₁H₄N₄O₂
Molecular Weight:224.18

Speicherung:

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

SMER3 Chemical Structure

CAS. Nr.: 67200-34-4

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

Biologische Aktivität

Beschreibung

SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF)^Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCF^Met30^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1 μM Compound: 1	Cytotoxicity against human A549 cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30508483]
A549/TR	IC₅₀	0.6 μM Compound: 1	Cytotoxicity against human A549/TR cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549/TR cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30508483]
L02	IC₅₀	14.3 μM Compound: 1	Cytotoxicity against NQO1 deficient human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against NQO1 deficient human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30508483]
LNCaP C4-2	IC₅₀	0.17 μM Compound: 7F1; LQZ-7F1	Cytotoxicity against human LNCaP C4-2 cells assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay Cytotoxicity against human LNCaP C4-2 cells assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay	[PMID: 35504208]
LNCaP C4-2	IC₅₀	0.17 μM Compound: 8; 7F1	Cytotoxicity against human LNCaP C4-2 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against human LNCaP C4-2 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 38092421]
LNCaP C4-2	IC₅₀	0.2 μM Compound: 7F1; LQZ-7F1	Cytotoxicity against human LNCaP C4-2 cells with empty vector-transfection assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay Cytotoxicity against human LNCaP C4-2 cells with empty vector-transfection assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay	[PMID: 35504208]
LNCaP C4-2	IC₅₀	0.95 μM Compound: 7F1; LQZ-7F1	Cytotoxicity against human LNCaP C4-2 cells with survivin overexpression assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay Cytotoxicity against human LNCaP C4-2 cells with survivin overexpression assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay	[PMID: 35504208]
PC-3	IC₅₀	0.16 μM Compound: 7F1; LQZ-7F1	Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay	[PMID: 35504208]
PC-3	IC₅₀	0.16 μM Compound: 8; 7F1	Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 38092421]

In Vitro

In yeast cells, Met4 ubiquitination is blocked in cells exposed to SMER3 (0-60 μM). The met4Δ cells are less susceptible to growth inhibition by SMER3^[1].
Addition of SMER3 to the ligase reactions inhibited ubiquitination of Met4 by SCF^Met30 in a dose-dependent manner. SMER3 significantly inhibits the binding of Met30 to Skp1, and does not affect the Skp1 and Met30 protein levels^[1].

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

Chemical Information

CAS. Nr. 67200-34-4
Appearance Solid
Molecular Weight 224.18
Formel C₁₁H₄N₄O₂
Color Light yellow to green yellow
SMILES

O=C1C2=NC3=NON=C3N=C2C4=C1C=CC=C4
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 : 12.5 mg/mL (55.76 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

4.4607 mL

22.3035 mL

44.6070 mL

5 mM

0.8921 mL

4.4607 mL

8.9214 mL

10 mM

0.4461 mL

2.2304 mL

4.4607 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: 1.25 mg/mL (5.58 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.

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 (277 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]. Mariam Aghajan, et al. Chemical genetics screen for enhancers of rapamycin identifies a specific inhibitor of an SCF family E3 ubiquitin ligase. Nat Biotechnol. 2010 Jul;28(7):738-42. [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	4.4607 mL	22.3035 mL	44.6070 mL	111.5175 mL
	5 mM	0.8921 mL	4.4607 mL	8.9214 mL	22.3035 mL
	10 mM	0.4461 mL	2.2304 mL	4.4607 mL	11.1518 mL
	15 mM	0.2974 mL	1.4869 mL	2.9738 mL	7.4345 mL
	20 mM	0.2230 mL	1.1152 mL	2.2304 mL	5.5759 mL
	25 mM	0.1784 mL	0.8921 mL	1.7843 mL	4.4607 mL
	30 mM	0.1487 mL	0.7435 mL	1.4869 mL	3.7173 mL
	40 mM	0.1115 mL	0.5576 mL	1.1152 mL	2.7879 mL
	50 mM	0.0892 mL	0.4461 mL	0.8921 mL	2.2304 mL

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SMER3

SZL P1-41

Pevonedistat

PRT4165

Y-27632 dihydrochloride

PR-619

Carfilzomib

Spautin-1

Heclin

PYR-41

Pomalidomide

NSC624206

Apcin

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

SMER3

SZL P1-41

Pevonedistat

PRT4165

Y-27632 dihydrochloride

PR-619

Carfilzomib

Spautin-1

Heclin

PYR-41

Pomalidomide

NSC624206

Apcin

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SMER3 Related Classifications

HY-10949 Related Classifications

Bioz