Synonym
SU16F; SU-16F; SU 16F;
IUPAC/Chemical Name
(Z)-3-[2,4-Dimethyl-5-(2-oxo-6-phenyl-1,2-dihydro-indol-3-ylidenemethyl)-1H-pyrrol-3-yl]-propionic acid
InChi Key
APYYTEJNOZQZNA-MOSHPQCFSA-N
InChi Code
InChI=1S/C24H22N2O3/c1-14-18(10-11-23(27)28)15(2)25-21(14)13-20-19-9-8-17(12-22(19)26-24(20)29)16-6-4-3-5-7-16/h3-9,12-13,25H,10-11H2,1-2H3,(H,26,29)(H,27,28)/b20-13-
SMILES Code
O=C(O)CCC1=C(C)NC(/C=C2C(NC3=C\2C=CC(C4=CC=CC=C4)=C3)=O)=C1C
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
To be determined
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
Excessively deposited fibrotic scar after spinal cord injury (SCI) inhibits axon regeneration. It has been reported that platelet-derived growth factor receptor beta (PDGFRβ), as a marker of fibrotic scar-forming fibroblasts, can only be activated by platelet-derived growth factor (PDGF) B or PDGFD. However, whether the activation of the PDGFRβ pathway can mediate fibrotic scar formation after SCI remains unclear.
Biological target:
SU16F is a PDGFRβ inhibitor with an IC50 value of 10 nM. It also inhibits VEGFR2 with an IC50 of 140 nM. SU16F selectively inhibits PDGF- over VEFG-, FGF-, and EGF-induced cell proliferation (IC50s = 0.11, 10, 10, and 21.9 μM, respectively).
In vitro activity:
SU1498 stimulated accumulation of phosphorylated ERKs in HUVECs and in human aortic endothelial cells, dependent on the functioning of the upstream components of the MAPK pathway, B-Raf, and MEK kinases. The enhanced accumulation of phospho-ERKs was observed only in cells that were stimulated with sphingosine 1-phosphate or protein growth factors; SU1498 alone was ineffective. SU1498 acted by blocking the kinase activity of phospho-ERK.
Reference: J Biol Chem. 2004 Feb 13;279(7):5716-24. https://pubmed.ncbi.nlm.nih.gov/14625306/
In vivo activity:
This study treated the mice after spinal cord injury (SCI) with SU16F and found reduction of fibrotic scar, interruption of scar boundary, and the inhibition of lesion and inflammation, which promoted axon regeneration and locomotor function recovery after SCI.
Reference: J Neuroinflammation. 2022 Apr 16;19(1):95. https://pubmed.ncbi.nlm.nih.gov/35429978/
Preparing Stock Solutions
The following data is based on the
product
molecular weight
386.45
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.
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. Li Z, Yu S, Liu Y, Hu X, Li Y, Xiao Z, Chen Y, Tian D, Xu X, Cheng L, Zheng M, Jing J. SU16f inhibits fibrotic scar formation and facilitates axon regeneration and locomotor function recovery after spinal cord injury by blocking the PDGFRβ pathway. J Neuroinflammation. 2022 Apr 16;19(1):95. doi: 10.1186/s12974-022-02449-3. PMID: 35429978; PMCID: PMC9013464.
2. Li Z, Zheng M, Yu S, Yao F, Luo Y, Liu Y, Tian D, Cheng L, Jing J. M2 Macrophages Promote PDGFRβ+ Pericytes Migration After Spinal Cord Injury in Mice via PDGFB/PDGFRβ Pathway. Front Pharmacol. 2021 Apr 15;12:670813. doi: 10.3389/fphar.2021.670813. PMID: 33935795; PMCID: PMC8082415.
In vitro protocol:
To be determined
In vivo protocol:
1. Li Z, Yu S, Liu Y, Hu X, Li Y, Xiao Z, Chen Y, Tian D, Xu X, Cheng L, Zheng M, Jing J. SU16f inhibits fibrotic scar formation and facilitates axon regeneration and locomotor function recovery after spinal cord injury by blocking the PDGFRβ pathway. J Neuroinflammation. 2022 Apr 16;19(1):95. doi: 10.1186/s12974-022-02449-3. PMID: 35429978; PMCID: PMC9013464.
2. Li Z, Zheng M, Yu S, Yao F, Luo Y, Liu Y, Tian D, Cheng L, Jing J. M2 Macrophages Promote PDGFRβ+ Pericytes Migration After Spinal Cord Injury in Mice via PDGFB/PDGFRβ Pathway. Front Pharmacol. 2021 Apr 15;12:670813. doi: 10.3389/fphar.2021.670813. PMID: 33935795; PMCID: PMC8082415.
1: Li Z, Yu S, Liu Y, Hu X, Li Y, Xiao Z, Chen Y, Tian D, Xu X, Cheng L, Zheng M, Jing J. SU16f inhibits fibrotic scar formation and facilitates axon regeneration and locomotor function recovery after spinal cord injury by blocking the PDGFRβ pathway. J Neuroinflammation. 2022 Apr 16;19(1):95. doi: 10.1186/s12974-022-02449-3. PMID: 35429978; PMCID: PMC9013464.
2: Li Z, Zheng M, Yu S, Yao F, Luo Y, Liu Y, Tian D, Cheng L, Jing J. M2 Macrophages Promote PDGFRβ+ Pericytes Migration After Spinal Cord Injury in Mice via PDGFB/PDGFRβ Pathway. Front Pharmacol. 2021 Apr 15;12:670813. doi: 10.3389/fphar.2021.670813. PMID: 33935795; PMCID: PMC8082415.
3: Diercke K, Kohl A, Lux CJ, Erber R. Compression of human primary cementoblasts leads to apoptosis: A possible cause of dental root resorption? J Orofac Orthop. 2014 Nov;75(6):430-45. doi: 10.1007/s00056-014-0237-5. Epub 2014 Oct 26. PMID: 25344124.
4: Huang F, Wang M, Yang T, Cai J, Zhang Q, Sun Z, Wu X, Zhang X, Zhu W, Qian H, Xu W. Gastric cancer-derived MSC-secreted PDGF-DD promotes gastric cancer progression. J Cancer Res Clin Oncol. 2014 Nov;140(11):1835-48. doi: 10.1007/s00432-014-1723-2. Epub 2014 Jun 18. PMID: 24938433.