Jk184 | JK-184 | CAS#315703-52-7 | hedgehog (Hh) signaling inhibitor

JK184
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406989

CAS#: 315703-52-7

Description: JK-184 is a potent downstream hedgehog (Hh) signaling inhibitor that prevents Gli-dependent transcriptional activity (IC50 = 30 nM). JK184 can specially inhibit Gli in the Hedgehog (Hh) pathway, which showed great promise for cancer therapeutics.

Chemical Structure

JK184

CAS# 315703-52-7

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406989
Name: JK184
CAS#: 315703-52-7
Chemical Formula: C19H18N4OS
Exact Mass: 350.12
Molecular Weight: 350.440
Elemental Analysis: C, 65.12; H, 5.18; N, 15.99; O, 4.57; S, 9.15

Price and Availability

Size	Price	Availability
50mg	USD 450
100mg	USD 750
200mg	USD 1250
500mg	USD 1950
1g	USD 2950	2 Weeks
2g	USD 5250	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

Appearance: 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:

Product Data:

Product Data

Instruction:

View handling instruction

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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	60.0	171.21
	Ethanol	14.0	39.95

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.

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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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