RepSox (Synonyms: E-616452; SJN 2511)

Name: RepSox
Brand: MedChemExpress
SKU: HY-13012
Rating: 5.0 (21 reviews)

Cat. No.: HY-13012 Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

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RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC₅₀ value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes.

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

RepSox Chemical Structure

CAS No. : 446859-33-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 85	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 85	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 385	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 660	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of RepSox:

RepSox (GMP) Get quote

20 Publications Citing Use of MCE RepSox

: RepSox purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jun 19;8(36):60159-60172. [Abstract]; SH-SY5Y (A) and HEK293 cells (B) are treated with 25 μM RepSox (Rep) in absence or presence of dPA or dPPA for 72 h, and the Western blotting results show that dPA or dPPA increases the expression in the presence of RepSox. RepSox does not cause significant alteration of furin protein compared to control. The expression of furin remains significantly increased after dPA or dPPA in the presence of RepSox.

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

ALK5

4 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
K562	IC₅₀	> 100 μM Compound: ALK5 inhibitor II	Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay	[PMID: 28135685]
MCF7	IC₅₀	> 100 μM Compound: ALK5 inhibitor II	Cytotoxicity against human MCF7 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay Cytotoxicity against human MCF7 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay	[PMID: 28135685]

In Vitro

RepSox (compound 19) inhibits ALK5 autophosphorylation with an IC₅₀ value of 4 nM^[1].
RepSox (0-10?μM; 0-8 days) induces adipogenesis from mouse embryonic fibroblasts (MEFs) in fibroblast culture medium^[2].
RepSox (0-10?μM; 0-8 days) promotes the differentiation of the brown fat precursor cells and induce browning of the white fat precursor cells^[2].
RepSox(0-10?μM; 0-8 days) induces brown adipogenesis in primary mouse fibroblasts and fat precursor cells^[2].

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

Western Blot Analysis^[2]

Cell Line:	Mouse embryonic fibroblasts (MEFs)
Concentration:	3 μM
Incubation Time:	0-8 days
Result:	Showed upregulation of UCP1 protein levels.

Immunofluorescence^[2]

Cell Line:	MEFs
Concentration:	3 μM
Incubation Time:	0-8 days
Result:	Increased the number of mitochondria in MEF-derived adipocytes and significantly increased UCP1 levels.

RT-PCR^[2]

Cell Line:	MEFs
Concentration:	3 μM
Incubation Time:	0-8 days
Result:	Induced the activation of a network of genes controlling adipogenesis, energy expenditure, and the thermogenic program in MEFs.

Molecular Weight

287.32

Formula

C₁₇H₁₃N₅

CAS No.

446859-33-2

Appearance

Solid

Color

Light brown to yellow

SMILES

CC1=NC(C2=NNC=C2C3=NC4=CC=CN=C4C=C3)=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (116.00 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	3.4804 mL	17.4022 mL	34.8044 mL
5 mM	0.6961 mL	3.4804 mL	6.9609 mL
10 mM	0.3480 mL	1.7402 mL	3.4804 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 7.5 mg/mL (26.10 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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: ≥ 7.5 mg/mL (26.10 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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.
Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 1.67 mg/mL (5.81 mM); Clear solution
Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (5.81 mM); Clear solution
Protocol 5

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.33 mg/mL (1.15 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.92%

Select Batch:

Data Sheet (281 KB) SDS (479 KB)

COA (253 KB) HNMR (241 KB) RP-HPLC (244 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)

References

[1]. Gellibert F, et al. Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. J Med Chem. 2004 Aug 26;47(18):4494-506. [Content Brief]

[2]. Wan-Zhi Tu, et al. RepSox, a small molecule inhibitor of the TGFβ receptor, induces brown adipogenesis and browning of white adipocytes. Acta Pharmacol Sin. 2019 Dec;40(12):1523-1531. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4804 mL	17.4022 mL	34.8044 mL	87.0110 mL
	5 mM	0.6961 mL	3.4804 mL	6.9609 mL	17.4022 mL
	10 mM	0.3480 mL	1.7402 mL	3.4804 mL	8.7011 mL
	15 mM	0.2320 mL	1.1601 mL	2.3203 mL	5.8007 mL
	20 mM	0.1740 mL	0.8701 mL	1.7402 mL	4.3505 mL
	25 mM	0.1392 mL	0.6961 mL	1.3922 mL	3.4804 mL
	30 mM	0.1160 mL	0.5801 mL	1.1601 mL	2.9004 mL
	40 mM	0.0870 mL	0.4351 mL	0.8701 mL	2.1753 mL
	50 mM	0.0696 mL	0.3480 mL	0.6961 mL	1.7402 mL
	60 mM	0.0580 mL	0.2900 mL	0.5801 mL	1.4502 mL
	80 mM	0.0435 mL	0.2175 mL	0.4351 mL	1.0876 mL
	100 mM	0.0348 mL	0.1740 mL	0.3480 mL	0.8701 mL

RepSox Related Classifications

Metabolic Disease

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.

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RepSox (Synonyms: E-616452; SJN 2511)

Customer Review

Other Forms of RepSox:

RepSox Related Antibodies

20 Publications Citing Use of MCE RepSox

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All TGF-β Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

RepSox Related Antibodies

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Complete Stock Solution Preparation Table

RepSox Related Classifications

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