Creative Biolabs

JK 184 [Hedgehog Inhibitor]

[CAT#: MOD2005ZP104]

Downstream Hedgehog signaling pathway inhibitor. Alcohol dehydrogenase 7 inhibitor.

Target:
Hedgehog

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Description
JK184 is a highly potent hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
Chemical Name
N-(4-Ethoxyphenyl)-4-(2-methylimida zo[1,2-a]pyridin-3-yl)-2-thiazolamine
Modulator Type
Inhibitor
Relevant Disease
Neurological Disorders
Assay Description
JK184 is designed to antagonize Hh signaling by inhibiting glioma (Gli)-dependent transcription activity in a dose-dependent manner. After three days of incubation, JK184 significantly inhibited the proliferation of HUVEC with IC50 of 6.3 μg/mL. In order to evaluate the antitumor effect of JK184, MTT analysis was performed in Panc-1 and BxPC-3 cells after administration of the specified concentration of compound, and the half-maximum inhibitory concentration (IC50) of JK184 (23.7 ng in anc-1 and 34.3 mL) ng / mL (in BxPC-3) [1]. Claudine low cell line is more sensitive to JK184 treatment than MCF10a, MTSV1-7 or HMLE-shGFP and HMLE-pBP cells, and JK184 induces glioma-related oncogene homolog 1 (GLI1) transcript and protein dose Dependence reduces the levels in these cells. Treatment with IC50 dose of JK184 can increase the proportion of HMLE-shEcad cells stained with Annexin-V but negative for propidium iodide (PI) (P<0.0001, t test) [2].
Reference
[1]. Zhang N, et al. Biodegradable polymeric micelles encapsulated JK184 suppress tumor growth through inhibiting Hedgehog signaling pathway. Nanoscale. 2015 Feb 14;7(6):2609-24.

[2]. Colavito SA, et al. 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.
Assay Description
JK184 (5 mg/kg, intravenous injection) shows good antiproliferative activity in the subcutaneous Panc-1 and BxPC-3 tumor models, and is a good candidate for anti-tumor drugs that target Hh signaling. However, JK184 has poor pharmacokinetics and bioavailability [1].
References
[1]. Zhang N, et al. Biodegradable polymeric micelles encapsulated JK184 suppress tumor growth through inhibiting Hedgehog signaling pathway. Nanoscale. 2015 Feb 14;7(6):2609-24.
Molecular Weight
350.44
Form
Powder
Chemical Formula
C19H18N4OS
Source
Synthetic
SMILES
CC2=C(C3=CSC(NC4=CC=C(OCC)C=C4)=N3)N1C=CC=CC1=N2
Solubility
Soluble in DMSO (100mM) or ethanol (25mM)
IC50
30 nM
CAS NO.
315703-52-7
PubChem Substance ID
1069686
Purity
>99%
Storage
Store at +4°C
Shipping
Room Temperature
Handling Advice
For obtaining a higher solubility, please warm the tube at 37 °C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -40°C for several months.
Research Use Only
For research use only
Target
Hedgehog
Official Name
Hedgehog
Full Name
Hedgehog
Alternative Names
Hh
Gene ID
6469(Human)
Uniprot ID
Q15465(Human)
For Research Use Only. Not For Clinical Use.
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