Toyocamycin

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

Toyocamycin 是放线菌产生的腺苷类似物，作为 XBP1 抑制剂，抑制 IRE1α 诱导的 ATP 依赖性 XBP1 mRNA 裂解 (IC50: 80 nM)。

Toyocamycin is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM). Toyocamycin induces apoptosis.

Western Blot Analysis Cell Line:HeLa, HEK293 Concentration:0, 0.03, 0.1, 0.3 μM Incubation Time:4 hours Result:Suppressed neither tunicamycin-induced ATF6 nor PERK activation.Inhibited IRE1α-induced XBP1 mRNA cleavage without affecting IRE1α phosphorylation on Ser724.Western Blot Analysis Cell Line:Human prostate cancer PC-3 cells Concentration:60 nM Incubation Time:12, 24, 36, 48 hours Result:Suppressed the phosphorylation level of AKA, while decreasing the phosphorylation level of ERK and p38. Cell Viability Assay Cell Line:PC-3 and RWPE-1 cells Concentration:0, 20, 40, 60, 80, 100 nM Incubation Time:24 or 48 hours Result:Inhibted cell viability and induced cell apoptosis by 62%.

Animal Model:SCID mice injected with human multiple myeloma (MM) cellsDosage:0.5 mg/kg, 1.0 mg/kg Administration:Intraperitoneal injection; twice a week; 2 weeks Result:Reduced the tumor volume significantly.Showed enhancing anti-tumor activity represented as smaller tumor volumes when compared with Bortezomib (HY-10227).

Vengicide

Others

Other Targets

XBP1

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606-58-6

291.26

C12H13N5O4

>98% (HPLC)

DMSO:100 mg/mL (343.34 mM; Need ultrasonic)

O[C@H]1[C@@H](O[C@H](CO)[C@H]1O)N2C3=C(C(N)=NC=N3)C(C#N)=C2

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(-20℃)

With Ice Pack

≥ 2 years