Synonym
JK-184; JK 184; JK184.
IUPAC/Chemical Name
N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)-2-thiazolamine
InChi Key
ROYXIPOUVGDTAO-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H18N4OS/c1-3-24-15-9-7-14(8-10-15)21-19-22-16(12-25-19)18-13(2)20-17-6-4-5-11-23(17)18/h4-12H,3H2,1-2H3,(H,21,22)
SMILES Code
CC1=C(C2=CSC(NC3=CC=C(OCC)C=C3)=N2)N4C=CC=CC4=N1
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:
JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
In vitro activity:
As shown in Figures 1(a) and S1A, B, the cell growth of all examined breast cancer cells was inhibited by JK184 in 24 hours, while MCF-10A cells showed higher tolerance to JK184. Additionally, EdU labeling (Figure 1(b)) and colony formation assay (Figure 1(c)) revealed that JK184 treatment resulted in marked proliferation inhibition in BCa cells. Taken together, these data reveal that JK184 shows a significant antitumor effect in BCa cells.
Reference: J Oncol. 2020 Jun 2;2020:1657896. https://pubmed.ncbi.nlm.nih.gov/32565796/
In vivo activity:
In addition, JK184 micelles exerted a sustained in vitro release behavior and had a stronger inhibitory effect on proliferation, migration and invasion of HUVECs than free JK184. Furthermore, JK184 micelles had stronger tumor growth inhibiting effects in subcutaneous Panc-1 and BxPC-3 tumor models.
Reference: Nanoscale. 2015 Feb 14;7(6):2609-24. https://pubmed.ncbi.nlm.nih.gov/25581613/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
60.0 |
171.21 |
| Ethanol |
14.0 |
39.95 |
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
350.44
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.
| 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. Xi X, He T. Inhibition of JK184-Induced Cytoprotective Autophagy Potentiates JK184 Antitumor Effects in Breast Cancer. J Oncol. 2020 Jun 2;2020:1657896. doi: 10.1155/2020/1657896. PMID: 32565796; PMCID: PMC7288248.
2. Oladapo HO, Tarpley M, Sauer SJ, Addo KA, Ingram SM, Strepay D, Ehe BK, Chdid L, Trinkler M, Roques JR, Darr DB, Fleming JM, Devi GR, Williams KP. Pharmacological targeting of GLI1 inhibits proliferation, tumor emboli formation and in vivo tumor growth of inflammatory breast cancer cells. Cancer Lett. 2017 Dec 28;411:136-149. doi: 10.1016/j.canlet.2017.09.033. Epub 2017 Sep 28. PMID: 28965853; PMCID: PMC5720365.
3. Zhang N, Liu S, Wang N, Deng S, Song L, Wu Q, Liu L, Su W, Wei Y, Xie Y, Gong C. Biodegradable polymeric micelles encapsulated JK184 suppress tumor growth through inhibiting Hedgehog signaling pathway. Nanoscale. 2015 Feb 14;7(6):2609-24. doi: 10.1039/c4nr06300g. PMID: 25581613.
In vitro protocol:
1. Xi X, He T. Inhibition of JK184-Induced Cytoprotective Autophagy Potentiates JK184 Antitumor Effects in Breast Cancer. J Oncol. 2020 Jun 2;2020:1657896. doi: 10.1155/2020/1657896. PMID: 32565796; PMCID: PMC7288248.
2. Oladapo HO, Tarpley M, Sauer SJ, Addo KA, Ingram SM, Strepay D, Ehe BK, Chdid L, Trinkler M, Roques JR, Darr DB, Fleming JM, Devi GR, Williams KP. Pharmacological targeting of GLI1 inhibits proliferation, tumor emboli formation and in vivo tumor growth of inflammatory breast cancer cells. Cancer Lett. 2017 Dec 28;411:136-149. doi: 10.1016/j.canlet.2017.09.033. Epub 2017 Sep 28. PMID: 28965853; PMCID: PMC5720365.
In vivo protocol:
1. Zhang N, Liu S, Wang N, Deng S, Song L, Wu Q, Liu L, Su W, Wei Y, Xie Y, Gong C. Biodegradable polymeric micelles encapsulated JK184 suppress tumor growth through inhibiting Hedgehog signaling pathway. Nanoscale. 2015 Feb 14;7(6):2609-24. doi: 10.1039/c4nr06300g. PMID: 25581613.
1: Zhang N, Liu S, Wang N, Deng S, Song L, Wu Q, Liu L, Su W, Wei Y, Xie Y, Gong
C. Biodegradable polymeric micelles encapsulated JK184 suppress tumor growth
through inhibiting Hedgehog signaling pathway. Nanoscale. 2015 Feb
14;7(6):2609-24. doi: 10.1039/c4nr06300g. PubMed PMID: 25581613.
2: Cupido T, Rack PG, Firestone AJ, Hyman JM, Han K, Sinha S, Ocasio CA, Chen JK.
The imidazopyridine derivative JK184 reveals dual roles for microtubules in
Hedgehog signaling. Angew Chem Int Ed Engl. 2009;48(13):2321-4. doi:
10.1002/anie.200805666. PubMed PMID: 19222062.
3: Colavito SA, Zou MR, Yan Q, Nguyen DX, Stern DF. Significance of
glioma-associated oncogene homolog 1 (GLI1) expression in claudin-low breast
cancer and crosstalk with the nuclear factor kappa-light-chain-enhancer of
activated B cells (NFκB) pathway. Breast Cancer Res. 2014 Sep 25;16(5):444. doi:
10.1186/s13058-014-0444-4. PubMed PMID: 25252859; PubMed Central PMCID:
PMC4303124.
4: Lee J, Wu X, Pasca di Magliano M, Peters EC, Wang Y, Hong J, Hebrok M, Ding S,
Cho CY, Schultz PG. A small-molecule antagonist of the hedgehog signaling
pathway. Chembiochem. 2007 Nov 5;8(16):1916-9. PubMed PMID: 17886323.
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