H4541

HPI-4

≥98% (HPLC)

• Synonim(y): 2,4-Dichloro-a-(3,4-dihydro-4-oxo-2(1H)-quinazolinylidene)-β-oxo-benzenepropanenitrile, Ciliobrevin A, Hedgehog Pathway Inhibitor 4
• Wzór empiryczny (zapis Hilla): C₁₇H₉Cl₂N₃O₂
• Numer CAS: 302803-72-1
• Masa cząsteczkowa: 358.18
• Numer MDL: MFCD01911757
• Kod UNSPSC: 51111800
• Identyfikator substancji w PubChem: 329815127
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥98% (HPLC)
• Postać: powder
• kolor: off-white, off-white to orange
• rozpuszczalność: DMSO: 10 mg/mL, clear
• temp. przechowywania: 2-8°C
• ciąg SMILES: Clc1ccc(c(Cl)c1)C(=O)\C(C#N)=C2\NC(=O)c3ccccc3N2
• InChI: 1S/C17H9Cl2N3O2/c18-9-5-6-10(13(19)7-9)15(23)12(8-20)16-21-14-4-2-1-3-11(14)17(24)22-16/h1-7,21H,(H,22,24)/b16-12+
• Klucz InChI: SESYPWCSIZUIAS-FOWTUZBSSA-N

Opis

Zastosowanie

Hedgehog pathway inhibitor (HP1-4) has been used for the inhibition of dynein ATPase in Leishmania.

Działania biochem./fizjol.

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.

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Informacja o środkach bezpieczeństwa

• Piktogramy: GHS07,GHS09
• Hasło ostrzegawcze: Warning
• Zwroty wskazujące rodzaj zagrożenia: H302,H410
• Zwroty wskazujące środki ostrożności: P264 - P270 - P273 - P301 + P312 - P391 - P501
• Klasyfikacja zagrożeń: Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1
• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable