JK 184 is a potent downstream hedgehog (Hh) signaling inhibitor that prevents Gli-dependent transcriptional activity (IC50 = 30 nM). Exhibits antiproliferative activity in a range of cancer cell lines (GI50 = 3 - 21 nM) and in human xenografts in vivo. Inhibits alcohol dehydrogenase 7 (Adh7) (IC50 = 210 nM) and acts as a microtubule depolymerizing agent in vitro.
| Molecular Weight | 350.44 |
| Formula | C19H18N4OS |
| CAS Number | 315703-52-7 |
| Solubility (25°C) | DMSO 35.04 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Hedgehog Products |
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TPB15 is an orally potent Hh (Hedgehog) signaling inhibitor that significantly induces MDA-MB-468 cell cycle arrest and apoptosis. TPB15 also blocks Smo (Smoothened) translocation into cilia and reduces Smo protein and mRNA expression. In addition, TPB15 can inhibit the expression of downstream regulator Glioma-associated oncogene 1 (Gli1). TPB15 has good anti-tumor activity and low toxicity. |
| Hedgehog IN-3
Hedgehog IN-3 is a hedgehog pathway inhibitor (IC50 = 0.01 µM). |
| Hedgehog IN-5
Hedgehog IN-5 is an orally active small molecule inhibitor of the hedgehog pathway. |
| Hedgehog IN-2
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| Physalin H
Physalin H is an inhibitor of Hedgehog (Hh) signaling and it disrupts GLI1-DNA-complex formation. Physalin H inhibits GLI1 transcription with an IC50 value of 0.7 μM. Physalin H shows cytotoxicity to PANC1 and DU145 cells with IC50 values of 5.7 and 6.8 μM, respectively. |
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