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RCM-1 339163-65-4

RCM-1 339163-65-4

CAS No.: 339163-65-4

RCM-1 is a novel and potent nontoxic FOXM1 inhibitor, which is able to inhibit goblet cell metaplasia and excessive mucu
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This product is for research use only, not for human use. We do not sell to patients.

RCM-1 is a novel and potent nontoxic FOXM1 inhibitor, which is able to inhibit goblet cell metaplasia and excessive mucus production.



Physicochemical Properties


Molecular Formula C20H12N2OS4
Molecular Weight 424.582078933716
Exact Mass 423.983
CAS # 339163-65-4
PubChem CID 4273985
Appearance Off-white to gray solid powder
LogP 5.6
Hydrogen Bond Donor Count 0
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 6
Heavy Atom Count 27
Complexity 580
Defined Atom Stereocenter Count 0
SMILES

S(CC(C1=CC=CS1)=O)C1=C(C#N)C(C2=CC=CS2)=CC(C2=CC=CS2)=N1

InChi Key DCCYTKKDAZEVLY-UHFFFAOYSA-N
InChi Code

InChI=1S/C20H12N2OS4/c21-11-14-13(17-4-1-7-24-17)10-15(18-5-2-8-25-18)22-20(14)27-12-16(23)19-6-3-9-26-19/h1-10H,12H2
Chemical Name

2-{[2-Oxo-2-(thiophen-2-yl)ethyl]sulfanyl}-4,6-di(thiophen-2-yl)pyridine-3- carbonitrile
Synonyms

RCM-1 RCM1 RCM 1.
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro RCM-1 inhibits FOXM1, a transcription factor essential for goblet cell development from airway progenitor cells, from nuclear localization and enhances its proteasomal degradation. RCM-1 inhibits the expression of the STAT6 target genes Spdef and Foxa3, which are important transcriptional regulators of goblet cell development, and decreases IL-13 and STAT6 signaling in cultured airway epithelial cells [1].
ln Vivo RCM-1 causes goblet cellization in mice exposed to home dust mites and interleukin 13 (IL-13). It does this by decreasing the production of proinflammatory cytokines, increasing lung compliance, and reducing airway resistance. RCM-1 suppresses IL-13 and STAT6 signaling in mice and inhibits the expression of the STAT6 target genes Foxa3 and Spdef [1].
References

[1]. The FOXM1 inhibitor RCM-1 suppresses goblet cell metaplasia and prevents IL-13 and STAT6 signaling in allergen-exposed mice. Sci Signal. 2017 Apr 18;10(475):eaai8583.


Solubility Data


Solubility (In Vitro) DMSO : ~16.67 mg/mL (~39.26 mM)
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)

Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3553 mL 11.7763 mL 23.5527 mL
5 mM 0.4711 mL 2.3553 mL 4.7105 mL
10 mM 0.2355 mL 1.1776 mL 2.3553 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.