PYR-41

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

PYR-41 是一种选择性、细胞渗透性泛素激活酶 (E1) 抑制剂。

PYR-41 is a selective, cell-permeable inhibitor of ubiquitin-activating enzyme (E1), blocks loading of immobilized His6-tagged E1 with ubiquitin with IC50 of <10 uM; does not affect the transfer of ubiquitin to E2 from E1, directly inhibits E1, but not E2; in addition to blocking ubiquitylation, PYR-41 increases total sumoylation in cells, attenuates cytokine-mediated nuclear factor-kappaB activation and inhibits nonproteasomal (Lys-63) ubiquitylation of TRAF6, also prevents the downstream ubiquitylation and proteasomal degradation of IκBα; inhibits degradation of p53 and activates the p53 transcriptional activity, demonstrates anti-tumor activity in animal studies.

PYR-41 increases total sumoylation in cells in addition to blocking ubiquitylation. PYR-41 attenuates cytokine-mediated nuclear factor-κB activation. PYR-41 also prevents the downstream ubiquitylation and proteasomal degradation of IκBα. Furthermore, PYR-41 inhibits degradation of p53 and activates the transcriptional activity of this tumor suppressor. PYR-41 (50?μM) promotes accumulation of ubiquitinated proteins. PYR-41 causes a concentration-dependent (10-50 μM) decline in DUB activity in Z138 cells after 4 h. PYR-41 potently inhibits USP5 DUB activity, even at the lowest concentration (10 μM). PYR-41 potently (10-50 μM) inhibits the activity of various DUBs, determined to represent USP9x, USP5, USP14, UCH37 and UCH-L3. Co-treatment of Z138 cells with DTT and PYR-41 completely abolishes the accumulation of ubiquitinated proteins.

——

PYR41 | PYR 41

Proteasome/Ubiquitin

E1

Ubiquitin-activatingEnzymeE1

Infection

——

418805-02-4

371.3

C17H13N3O7

>98% (HPLC)

DMSO: ≥ 46 mg/mL

O=C(OCC)C1=CC=C(N2NC(/C(C2=O)=C/C3=CC=C([N+]([O-])=O)O3)=O)C=C1

Benzoic acid, 4-[4-[(5-nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]-, ethyl ester

(-20℃)

With Ice Pack

≥ 2 years