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Chemical Structure| 315703-52-7 Chemical Structure| 315703-52-7

Structure of JK184
CAS No.: 315703-52-7

Chemical Structure| 315703-52-7

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JK184 is a hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.

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Product Details of JK184

CAS No. :315703-52-7
Formula : C19H18N4OS
M.W : 350.44
SMILES Code : CC1=C(C2=CSC(NC3=CC=C(OCC)C=C3)=N2)N4C=CC=CC4=N1
MDL No. :MFCD01044465
InChI Key :ROYXIPOUVGDTAO-UHFFFAOYSA-N
Pubchem ID :1069686

Safety of JK184

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
SUM159 30 nM 72 hours JK184 significantly reduced SUM159 cell proliferation and inhibited GLI1 mRNA expression Cancer Lett. 2017 Dec 28;411:136-149
MDA-MB-231 30 nM 72 hours JK184 significantly reduced MDA-MB-231 cell proliferation and inhibited GLI1 mRNA expression Cancer Lett. 2017 Dec 28;411:136-149
SUM149 30 nM 72 hours JK184 significantly reduced SUM149 cell proliferation and inhibited GLI1 mRNA expression Cancer Lett. 2017 Dec 28;411:136-149
HCT116 cells 1 μM 24 hours JK184 induced apoptosis in HCT116 cells, with an apoptosis rate of approximately 28.8%. J Transl Med. 2023 Jan 13;21(1):23
MDA-MB-231 cells 1 μM 24 hours JK184 induced apoptosis in MDA-MB-231 cells, with an apoptosis rate of approximately 42.04%. J Transl Med. 2023 Jan 13;21(1):23
MDA.MB.436 cells 0.002 μM 72 hours JK184 inhibited the proliferation of MDA.MB.436 cells and reduced GLI1 transcript and protein levels. Breast Cancer Res. 2014 Sep 25;16(5):444
BT549 cells 0.002 μM 72 hours JK184 inhibited the proliferation of BT549 cells and reduced GLI1 transcript and protein levels. Breast Cancer Res. 2014 Sep 25;16(5):444
HMLE-Snail cells 0.004 μM 72 hours JK184 inhibited the proliferation of HMLE-Snail cells and reduced GLI1 transcript and protein levels. Breast Cancer Res. 2014 Sep 25;16(5):444
HMLE-shEcad cells 0.004 μM 72 hours JK184 inhibited the proliferation of HMLE-shEcad cells and reduced GLI1 transcript and protein levels. Breast Cancer Res. 2014 Sep 25;16(5):444
Hep2 cells 10 μM 48 hours To evaluate the effect of JK184 alone or in combination with shEGFR on the viability of Hep2 cells. Results showed that the combination of JK184 and shEGFR significantly reduced cell viability. Int J Clin Exp Pathol. 2017 Sep 1;10(9):9816-9828
FaDu cells 10 μM 48 hours To evaluate the effect of JK184 alone or in combination with shEGFR on the viability of FaDu cells. Results showed that the combination of JK184 and shEGFR significantly reduced cell viability and induced a higher apoptosis rate. Int J Clin Exp Pathol. 2017 Sep 1;10(9):9816-9828
786-O cells 10 nM 48 hours Inhibited the Hedgehog signaling pathway, decreased the expression levels of SHH, SMO, and GLi1, and increased the expression levels of PTCH2 and SUFU. Cancer Cell Int. 2023 Dec 12;23(1):319
B7-H3 CAR T cells 1 μM 24 hours JK184 modulates B7-H3 CAR T cells to an effector memory phenotype and promotes cytokine secretion. J Transl Med. 2023 Jan 13;21(1):23

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
M-NSG mice MDA-MB-231-FFluc and HCT116-FFluc xenograft models Intraperitoneal injection 5 mg/kg 10 consecutive days JK184 combined with B7-H3 CAR T cells significantly inhibited tumor growth and prolonged survival in mice. J Transl Med. 2023 Jan 13;21(1):23
Balb/c nude mice Maxillary sinus tumor model Subcutaneous injection 10 mg/kg body weight Three times a week, continuous treatment To evaluate the inhibitory effect of JK184 alone or in combination with shEGFR on tumor growth. Results showed that the inhibitory rate of the combined therapy was significantly higher than that of single treatments. Int J Clin Exp Pathol. 2017 Sep 1;10(9):9816-9828

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.27mL

2.85mL

1.43mL

28.54mL

5.71mL

2.85mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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