Marizomib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的口服生物活性 20S 蛋白酶体抑制剂，IC50 为 1.3 nM。

A potent, orally bioactive 20S proteasome inhibitor with IC50 of 1.3 nM (inhibition of proteasomal chymotrypsin-like proteolytic activity); displays 35 times more potent than omuralide; induces apoptosis in multiple myeloma cells with mechanisms distinct from Bortezomib, including chemical structure, effects on proteasome activities, mechanisms of action, and toxicity profile against normal cells; significantly reduces tumor recurrence in animal tumor model studies.Blood Cancer Phase 2 Clinical.

Marizomib (Salinosporamide A) (0.1-10000 nM; 72 hours) effectively reduces survival of D-54 and U-251 cells in a dose-dependent manner. The IC50s are ～52 nM for U-251 and ～20 nM for D-54.Marizomib (24 hours; 60 nM) induces apoptosis and caspase-3 activation in glioma cells. Cell Proliferation AssayCell Line:U-251 and D-54 cells Concentration:0.1, 1, 10, 100, 1000, 10000 nM Incubation Time:72 hours Result:Effectively reduced survival of D-54 and U-251 cells in a dose-dependent manner.Apoptosis Analysis Cell Line:D-54 cells Concentration:60 nM Incubation Time:24 hours Result:Induces D-54 cells apoptosis.Western Blot Analysis Cell Line:D-54 cellsConcentration:60 nMIncubation Time:24 hoursResult:Led to increased activity of caspase-3 in a dose-dependent manner.

Marizomib (Salinosporamide A) (0.15 mg/kg; i.v; twice a week for three weeks) significantly decreases tumor growth, and is not associated with any toxicity. Animal Model:CB-17 SCID-male mice (4-6 weeks old)Dosage:0.15 mg/kgAdministration:i.v; twice a week for three weeks Result:Significantly decreased tumor growth, and was not associated with any toxicity.

NPI 0052 | Salinosporamide A

Proteasome/Ubiquitin

Proteasome

Proteasome

Cancer

Blood cancer

437742-34-2

313.781

C15H20ClNO4

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (318.69 mM)

C[C@]12[C@H](C(=O)N[C@]1(C(=O)O2)[C@H]([C@H]3CCCC=C3)O)CCCl

(1R,4R,5S)-4-(2-Chloroethyl)-1-[(S)-(1S)-2-cyclohexen-1-ylhydroxymethyl]-5-methyl-6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dione

(-20℃)

With Ice Pack

≥ 2 years