HPI-4,Hedgehog Pathway Inhibitor 4 Struktur

HPI-4,Hedgehog Pathway Inhibitor 4

Bezeichnung:HPI-4,Hedgehog Pathway Inhibitor 4

CAS-Nr302803-72-1

Englisch Name:HPI-4,Hedgehog Pathway Inhibitor 4

CBNumberCB72644957

SummenformelC17H9Cl2N3O2

Molgewicht358.18

MOL-Datei302803-72-1.mol

HPI-4,Hedgehog Pathway Inhibitor 4 physikalisch-chemischer Eigenschaften

Siedepunkt	564.5±50.0 °C(Predicted)
Dichte	1.471±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: soluble10mg/mL, clear
pka	6.46±0.20(Predicted)
Aggregatzustand	powder
Farbe	off-white, off-white to orange

Sicherheit

Kennzeichnung gefährlicher	Xn,N
R-Sätze:	22-50/53
S-Sätze:	60-61
RIDADR	UN 3077 9 / PGIII
WGK Germany	3

Gefahreninformationscode (GHS)

HPI-4,Hedgehog Pathway Inhibitor 4 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Ciliobrevin A is a hedgehog pathway inhibitor that blocks sonic hedgehog (Shh)-induced hedgehog pathway activation (IC₅₀ = 7 μM). It disrupts primary cilia formation and inhibits the dynein-dependent microtubial gliding and ATPase activities of the cytoplasmic ATPases associated with various cellular activities (AAA+) family. Ciliobrevin A also inhibits mammalian target of rapamycin complex 1 (mTORC1) activity in uninfected and human cytomegalovirus (HCMV)-infected cells, suggesting that mTORC1 activation requires dynein-dependent transport for cellular activation.
Verwenden
Ciliobrevin A is a Hedgehog pathway inhibitor; ciliogenesis inhibitor. The Hedgehog (HH) signaling pathway is targeted for anti-cancer therapeutics. Ciliobrevin A inhibited proliferation of cerebellar granula neuron precursor cells, an important model of HH signaling.
Verwenden
Hedgehog pathway inhibitor (HP1-4) has been used for the inhibition of dynein ATPase in Leishmania.
Biochem/physiol Actions
HPI-4 is a Hedgehog pathway inhibitor; ciliogenesis inhibitor. The Hedgehog (HH) signaling pathway is targeted for anti-cancer therapeutics. A key signaling molecule in HH pathway, Smoothened (Smo), has been the target of pharmacological intervention, which has resulted in multiple Smo antagonists including Cyclopamine. However, the oncogenic form of Smo is resistant to Cyclopamine, so the identification of inhibitors of downstream effectors, such as the transcription factors Gli1 and Gli2, is important. Four small molecules were identified to inhibit HH downstream of Smo, HPI-1, HPI-2, HPI-3, and HPI-4. HPI-4 blocked HH pathway activation by SAG, decreased Smo ciliary accumulation, decreased HH activity in a consitutively active HH cell line, and decreased Gli1 and Gli2, processing, and stability. HPI-4 inhibited proliferation of cerebellar granula neuron precursor cells, an important model of HH signaling. Cilia in HPI-4-treated cells were either truncated or absent. The mechanism of action of HPI-4 is hypothesized to be directly through perturbation of ciliogenesis, leading to disruption of Gli1/Gli2 activity, which is distinctly different from that of Cyclopamine.
Lager
Store at +4°C

HPI-4,Hedgehog Pathway Inhibitor 4 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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