Synonym
FDI-6; FDI 6; FDI6; NCGC00099374; NCGC-00099374; NCGC 00099374; Forkhead Domain Inhibitory Compound 6
IUPAC/Chemical Name
3-Amino-N-(4-fluorophenyl)-6-thiophen-2-yl-4-(trifluoromethyl)thieno[2,3-b]pyridine-2-carboxamide
InChi Key
ZATJMMZPGVDUOM-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H11F4N3OS2/c20-9-3-5-10(6-4-9)25-17(27)16-15(24)14-11(19(21,22)23)8-12(26-18(14)29-16)13-2-1-7-28-13/h1-8H,24H2,(H,25,27)
SMILES Code
O=C(C1=C(N)C2=C(C(F)(F)F)C=C(C3=CC=CS3)N=C2S1)NC4=CC=C(F)C=C4
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
Biological target:
FDI-6 is an inhibitor of FOXM1.
In vitro activity:
This study then investigated the anti-proliferative effect of FDI-6 using a Sulforhodamine B (SRB) assay. The results demonstrated that FDI-6 inhibits cell proliferation in a dose-dependent manner.
Reference: Int J Mol Sci. 2021 Jun 22;22(13):6685. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8269391/
In vivo activity:
In vivo, FDI-6 (40 μM) was injected subconjunctivally to a rabbit trabeculectomy model. The results showed that, in cell culture studies, FDI-6 suppressed the proliferation, migration, collagen gel contraction and the expression levels of fibronectin (FN) and α-smooth muscle actin (α-SMA) in RTFs with TGF-β treatment by down-regulating the TGF-β1/Smad2/3 signaling pathway. In animal studies, the IOPs of the FDI-6-treated group were significantly lower than those of the saline-treated group after trabeculectomy. The FDI-6-treated eyes showed a better bleb appearance with fewer blood vessels compared to the saline-treated eyes.
Reference: Exp Eye Res. 2021 Aug 7:108725. https://pubmed.ncbi.nlm.nih.gov/34375589/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
64.3 |
147.09 |
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
437.43
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. Ulhaka K, Kanokwiroon K, Khongkow M, Bissanum R, Khunpitak T, Khongkow P. The Anticancer Effects of FDI-6, a FOXM1 Inhibitor, on Triple Negative Breast Cancer. Int J Mol Sci. 2021 Jun 22;22(13):6685. doi: 10.3390/ijms22136685. PMID: 34206484; PMCID: PMC8269391.
2. Liu Y, Zhu L, Wen T, Wan J, Lei Y, Chen H. [Forkhead domain inhibitor-6 (FDI-6) increases apoptosis and inhibits invasion and migration of laryngeal carcinoma cells by down-regulating nuclear FoxM1]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2017 May;33(5):611-616. Chinese. PMID: 28502298.
3. Lan C, Tan J, Tang L, Liu G, Huang L, Luo X, Zhou L, Zhu Y, Liu X, Fan N. Forkhead domain inhibitory-6 attenuates subconjunctival fibrosis in rabbit model with trabeculectomy. Exp Eye Res. 2021 Aug 7:108725. doi: 10.1016/j.exer.2021.108725. Epub ahead of print. PMID: 34375589.
In vitro protocol:
1. Ulhaka K, Kanokwiroon K, Khongkow M, Bissanum R, Khunpitak T, Khongkow P. The Anticancer Effects of FDI-6, a FOXM1 Inhibitor, on Triple Negative Breast Cancer. Int J Mol Sci. 2021 Jun 22;22(13):6685. doi: 10.3390/ijms22136685. PMID: 34206484; PMCID: PMC8269391.
2. Liu Y, Zhu L, Wen T, Wan J, Lei Y, Chen H. [Forkhead domain inhibitor-6 (FDI-6) increases apoptosis and inhibits invasion and migration of laryngeal carcinoma cells by down-regulating nuclear FoxM1]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2017 May;33(5):611-616. Chinese. PMID: 28502298.
In vivo protocol:
1. Lan C, Tan J, Tang L, Liu G, Huang L, Luo X, Zhou L, Zhu Y, Liu X, Fan N. Forkhead domain inhibitory-6 attenuates subconjunctival fibrosis in rabbit model with trabeculectomy. Exp Eye Res. 2021 Aug 7:108725. doi: 10.1016/j.exer.2021.108725. Epub ahead of print. PMID: 34375589.
1: Tabatabaei-Dakhili SA, Aguayo-Ortiz R, Domínguez L, Velázquez-Martínez CA. Untying the knot of transcription factor druggability: Molecular modeling study of FOXM1 inhibitors. J Mol Graph Model. 2018 Mar;80:197-210. doi: 10.1016/j.jmgm.2018.01.009. Epub 2018 Jan 31. PubMed PMID: 29414039.
2: Otto-Duessel M, Tew BY, Vonderfecht S, Moore R, Jones JO. Identification of neuron selective androgen receptor inhibitors. World J Biol Chem. 2017 May 26;8(2):138-150. doi: 10.4331/wjbc.v8.i2.138. PubMed PMID: 28588757; PubMed Central PMCID: PMC5439165.
3: Liu Y, Zhu L, Wen T, Wan J, Lei Y, Chen H. [Forkhead domain inhibitor-6 (FDI-6) increases apoptosis and inhibits invasion and migration of laryngeal carcinoma cells by down-regulating nuclear FoxM1]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2017 May;33(5):611-616. Chinese. PubMed PMID: 28502298.
4: Youn M, Wang N, LaVasseur C, Bibikova E, Kam S, Glader B, Sakamoto KM, Narla A. Loss of Forkhead box M1 promotes erythropoiesis through increased proliferation of erythroid progenitors. Haematologica. 2017 May;102(5):826-834. doi: 10.3324/haematol.2016.156257. Epub 2017 Feb 2. PubMed PMID: 28154085; PubMed Central PMCID: PMC5477601.
5: Marsico G, Gormally MV. Small molecule inhibition of FOXM1: How to bring a novel compound into genomic context. Genom Data. 2014 Oct 22;3:19-23. doi: 10.1016/j.gdata.2014.10.012. eCollection 2015 Mar. PubMed PMID: 26484143; PubMed Central PMCID: PMC4535965.
6: Kalinichenko VV, Kalin TV. Is there potential to target FOXM1 for 'undruggable' lung cancers? Expert Opin Ther Targets. 2015 Jul;19(7):865-7. doi: 10.1517/14728222.2015.1042366. Epub 2015 May 4. PubMed PMID: 25936405; PubMed Central PMCID: PMC4836176.
7: Gormally MV, Dexheimer TS, Marsico G, Sanders DA, Lowe C, Matak-Vinković D, Michael S, Jadhav A, Rai G, Maloney DJ, Simeonov A, Balasubramanian S. Suppression of the FOXM1 transcriptional programme via novel small molecule inhibition. Nat Commun. 2014 Nov 12;5:5165. doi: 10.1038/ncomms6165. PubMed PMID: 25387393; PubMed Central PMCID: PMC4258842.
8: Ridding MC, Taylor JL, Rothwell JC. The effect of voluntary contraction on cortico-cortical inhibition in human motor cortex. J Physiol. 1995 Sep 1;487 ( Pt 2):541-8. PubMed PMID: 8558482; PubMed Central PMCID: PMC1156591.
