GSK3494245 - ≥98% , CAS No.2080410-41-7

CAS: 2080410-41-7 Cat. No.: G651772 Summenformel: C₂₁H₂₃FN₆O₂ Molekulargewicht: 410.44 PubChem CID: 126571915

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Übersicht

GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits ( IC 50 =0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC 50 : purified 26S=13 µM; enriched THP-1 extracts IC 50 =40µM). GSK3494245 exhibits attractive biological and biosafety properties.

In Vitro

GSK3494245 shows EC 50 value of 5.7 μM in L. donovani intramacrophage assay, where the amastigotes are cultured in differentiated THP-1 cells. GSK3494245 demonstrates good selectivity over mammalian cell growth inhibition (THP-1 cells; EC 50 > 50 μM). GSK3494245 (DDD01305143) shows pEC 50 s of 6.5 and 5.8 against axenic amastigote and ld InMac, respectively. Ld InMac is the intramacrophage assay carried out in THP-1 cells with L. donovani amastigote. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GSK3494245 (25 mg/kg; orally twice a day for 10 consecutive days) elicits a >95% reduction of parasite load in Infected mice ( L. donovani , LV9) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

Specifications

Spezifikationen & Reinheit

≥98%

Biochemische und physiologische Mechanismen

GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits ( IC 50 =0.16 μM for WT L. donovani proteasomes). GSK3494

Storage

Store at -20°C

Verschickt in

Ice chest + Ice pads

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

INHIBITOR

Reinheit

≥98%

Namen und Kennungen

Isomere SMILES

C1CCN(C1)C(=O)NC2=CC(=C(C=C2)F)C3=NC4=NC=C(N4C=C3)N5CCOCC5

PubChem CID

126571915

Molekulargewicht

410.44

Zugehörige Ziele (menschlich)

LCK Tclin Tyrosine-protein kinase LCK (9212 Activities)

Discover Target: LCK

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 Activities)

Discover Target: AURKB

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PIK3CG Tclin PI3-kinase p110-gamma subunit (5411 Activities)

Discover Target: PIK3CG

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Zugehörige Ziele (nicht menschlich)

Leishmania donovani (89745 Activities)

Explore this target

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Wirkungsmechanismen

Chemische und physikalische Eigenschaften

• Löslichkeit: DMSO : 100 mg/mL (243.64 mM; Need ultrasonic)

Häufig gestellte Fragen

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2080410-41-7, the molecular formula is C21H23FN6O2, and the molecular weight is 410.44 g/mol.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.