MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 406988 | Name: RhoA-IN-Y16
Featured New

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Y16, also known as RhoA-IN-Y16, is a RhoA inhibitor, Y16 blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM). Y16 specifically inhibits LARG catalyzed activation of RhoA and RhoA signaling pathways. Y16 blocks the growth and migration of MCF7 breast cancer cells.

Chemical Structure

RhoA-IN-Y16
RhoA-IN-Y16
CAS#429653-73-6

Theoretical Analysis

MedKoo Cat#: 406988

Name: RhoA-IN-Y16

CAS#: 429653-73-6

Chemical Formula: C24H20N2O3

Exact Mass: 384.1474

Molecular Weight: 384.44

Elemental Analysis: C, 74.98; H, 5.24; N, 7.29; O, 12.49

Price and Availability

Size Price Availability Quantity
5mg USD 90.00 Ready to Ship
10mg USD 150.00 Ready to Ship
25mg USD 250.00 Ready to Ship
50mg USD 450.00 Ready to Ship
100mg USD 750.00 Ready to Ship
200mg USD 1,350.00 Ready to Ship
Show More
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
No Data
Synonym
RhoA-IN-Y16; Y16; Y-16; Y 16.
IUPAC/Chemical Name
(E)-4-(3-((3-methylbenzyl)oxy)benzylidene)-1-phenylpyrazolidine-3,5-dione
InChi Key
ITMLWGWTDWJSRZ-PXLXIMEGSA-N
InChi Code
InChI=1S/C24H20N2O3/c1-17-7-5-9-19(13-17)16-29-21-12-6-8-18(14-21)15-22-23(27)25-26(24(22)28)20-10-3-2-4-11-20/h2-15H,16H2,1H3,(H,25,27)/b22-15+
SMILES Code
O=C(/C1=C\C2=CC=CC(OCC3=CC=CC(C)=C3)=C2)NN(C4=CC=CC=C4)C1=O
Appearance
Orange to yellow solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM.
In vitro activity:
In cells, Y16 selectively inhibits serum-induced RhoA activity and RhoA-mediated signaling, effects that can be rescued by a constitutively active RhoA or ROCK mutant. By suppressing RhoA activity, Y16 inhibits mammary sphere formation of MCF7 breast cancer cells but does not affect the nontransforming MCF10A cells. Reference: Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60. https://pubmed.ncbi.nlm.nih.gov/23382194/
In vivo activity:
Animal xenograft models were used to investigate antitumor effects after ARHGEF12 knockdown or treatment with the ARHGEF12 inhibitor Y16 in vivo. Targeting ARHGEF12 with the small molecular inhibitor Y16 induced cell differentiation and attenuated neuroblastoma tumorigenicity. Reference: Cell Oncol (Dordr). 2022 Dec 15. https://pubmed.ncbi.nlm.nih.gov/36520365/
Solvent mg/mL mM
Solubility
DMSO 32.0 83.24
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 384.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Shang X, Marchioni F, Evelyn CR, Sipes N, Zhou X, Seibel W, Wortman M, Zheng Y. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60. doi: 10.1073/pnas.1212324110. Epub 2013 Feb 4. PMID: 23382194; PMCID: PMC3581902. 2. Chiu WC, Chiang JY, Chiang FT. Small chemical compounds Y16 and Rhosin can inhibit calcium sensitization pathway in vascular smooth muscle cells of spontaneously hypertensive rats. J Formos Med Assoc. 2021 Oct;120(10):1863-1868. doi: 10.1016/j.jfma.2021.03.031. Epub 2021 Apr 21. PMID: 33893012. 3. Yang Y, Wang S, Cai J, Liang J, Zhang Y, Xie Y, Luo F, Tang J, Gao Y, Shen S, Feng H, Li Y. Targeting ARHGEF12 promotes neuroblastoma differentiation, MYCN degradation, and reduces tumorigenicity. Cell Oncol (Dordr). 2022 Dec 15. doi: 10.1007/s13402-022-00739-9. Epub ahead of print. PMID: 36520365.
In vitro protocol:
1. Shang X, Marchioni F, Evelyn CR, Sipes N, Zhou X, Seibel W, Wortman M, Zheng Y. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60. doi: 10.1073/pnas.1212324110. Epub 2013 Feb 4. PMID: 23382194; PMCID: PMC3581902. 2. Chiu WC, Chiang JY, Chiang FT. Small chemical compounds Y16 and Rhosin can inhibit calcium sensitization pathway in vascular smooth muscle cells of spontaneously hypertensive rats. J Formos Med Assoc. 2021 Oct;120(10):1863-1868. doi: 10.1016/j.jfma.2021.03.031. Epub 2021 Apr 21. PMID: 33893012.
In vivo protocol:
1. Yang Y, Wang S, Cai J, Liang J, Zhang Y, Xie Y, Luo F, Tang J, Gao Y, Shen S, Feng H, Li Y. Targeting ARHGEF12 promotes neuroblastoma differentiation, MYCN degradation, and reduces tumorigenicity. Cell Oncol (Dordr). 2022 Dec 15. doi: 10.1007/s13402-022-00739-9. Epub ahead of print. PMID: 36520365.
1: Chiu WC, Chiang JY, Chiang FT. Small chemical compounds Y16 and Rhosin can inhibit calcium sensitization pathway in vascular smooth muscle cells of spontaneously hypertensive rats. J Formos Med Assoc. 2021 Oct;120(10):1863-1868. doi: 10.1016/j.jfma.2021.03.031. Epub 2021 Apr 21. PMID: 33893012. 2: Dhanasekaran S, Yang Q, Godana EA, Liu J, Li J, Zhang H. Trehalose supplementation enhanced the biocontrol efficiency of Sporidiobolus pararoseus Y16 through increased oxidative stress tolerance and altered transcriptome. Pest Manag Sci. 2021 Oct;77(10):4425-4436. doi: 10.1002/ps.6477. Epub 2021 May 28. PMID: 33987938. 3: Zhang SM, Li WG, Zhang DY, Huang XF, Qin W, Sha CQ. Purification and characterization of a low-temperature hydroxylamine oxidase from heterotrophic nitrifier Acinetobacter sp. Y16. Biomed Environ Sci. 2014 Jul;27(7):515-22. doi: 10.3967/bes2014.004. PMID: 25073910. 4: Huang X, Li W, Zhang D, Qin W. Ammonium removal by a novel oligotrophic Acinetobacter sp. Y16 capable of heterotrophic nitrification-aerobic denitrification at low temperature. Bioresour Technol. 2013 Oct;146:44-50. doi: 10.1016/j.biortech.2013.07.046. Epub 2013 Jul 18. PMID: 23911816. 5: Begg KJ, Tomoyasu T, Donachie WD, Khattar M, Niki H, Yamanaka K, Hiraga S, Ogura T. Escherichia coli mutant Y16 is a double mutant carrying thermosensitive ftsH and ftsI mutations. J Bacteriol. 1992 Apr;174(7):2416-7. doi: 10.1128/jb.174.7.2416-2417.1992. PMID: 1551860; PMCID: PMC205870. 6: Boateng NAS, Ackah M, Wang K, Dzah CS, Zhang H. Comparative physiological and transcriptomic analysis reveals an improved biological control efficacy of Sporidiobolus pararoseus Y16 enhanced with ascorbic acid against the oxidative stress tolerance caused by Penicillium expansum in pears. Plant Physiol Biochem. 2024 May;210:108627. doi: 10.1016/j.plaphy.2024.108627. Epub 2024 Apr 19. PMID: 38663265. 7: Hamid S, Ahmad I, Akhtar MJ, Iqbal MN, Shakir M, Tahir M, Rasool A, Sattar A, Khalid M, Ditta A, Zhu B. Bacillus subtilis Y16 and biogas slurry enhanced potassium to sodium ratio and physiology of sunflower (Helianthus annuus L.) to mitigate salt stress. Environ Sci Pollut Res Int. 2021 Aug;28(29):38637-38647. doi: 10.1007/s11356-021-13419-2. Epub 2021 Mar 18. Erratum in: Environ Sci Pollut Res Int. 2021 Aug;28(29):38648. doi: 10.1007/s11356-021-14344-0. PMID: 33735413. 8: Hamid S, Ahmad I, Akhtar MJ, Iqbal MN, Shakir M, Tahir M, Rasool A, Sattar A, Khalid M, Ditta A, Zhu B. Correction to: Bacillus subtilis Y16 and biogas slurry enhanced potassium to sodium ratio and physiology of sunflower (Helianthus annuus L.) to mitigate salt stress. Environ Sci Pollut Res Int. 2021 Aug;28(29):38648. doi: 10.1007/s11356-021-14344-0. Erratum for: Environ Sci Pollut Res Int. 2021 Aug;28(29):38637-38647. doi: 10.1007/s11356-021-13419-2. PMID: 33970423. 9: Kim TJ, Nam KW, Kim B, Lee SJ, Oh KB, Kim KH, Mar W, Shin J. Inhibitory effects of costunolide isolated from Laurus nobilis on IgE-induced degranulation of mast cell-like RBL-2H3 cells and the growth of Y16 pro-B cells. Phytother Res. 2011 Sep;25(9):1392-7. doi: 10.1002/ptr.3553. Epub 2011 Jun 14. PMID: 21674633. 10: Ackah M, Boateng NAS, Dhanasekaran S, Zhang H, Yang Q. Genome wide and comprehensive analysis of the cytochrome P450 (CYPs) gene family in Pyrus bretschneideri: Expression patterns during Sporidiobolus pararoseus Y16 enhanced with ascorbic acid (VC) treatment. Plant Physiol Biochem. 2024 Jan;206:108303. doi: 10.1016/j.plaphy.2023.108303. Epub 2023 Dec 22. PMID: 38154299.