Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6041 |
Oprozomib
PR-047,奥泼佐米,ONX 0912 |
Proteasome; Autophagy | Autophagy; Proteases/Proteasome; Ubiquitination |
Oprozomib (PR-047) 是一种可口服的选择性肽环氧酮类蛋白酶体抑制剂,诱导多发性骨髓瘤细胞凋亡。它对蛋白酶体 (β5) 和免疫蛋白酶体 (LMP7) 的 IC50分别为 36 和 82 nM。 | |||
T6029 |
ONX-0914
ONX0914,PR-957,ONX 0914 |
Proteasome; HIV Protease; Antibacterial | Microbiology/Virology; Proteases/Proteasome; Ubiquitination |
ONX-0914 (PR-957) 是选择性的低分子量多肽-7(LMP7)的抑制剂,LMP7 是免疫蛋白酶体的类糜蛋白酶亚单位。它是分枝杆菌蛋白酶体的非竞争性不可逆抑制剂,Ki 值为5.2 μM。它通过 HSF-1 介导的 p-TEFb 活化激活潜伏的 HIV-1。 | |||
T37420 |
Ac-ANW-AMC
Ac-ANW-AMC,Ac-Ala-Asn-Trp-AMC |
||
Ac-ANW-AMC is a fluorogenic substrate for the β5i/LMP7 subunit of the 20S immunoproteasome. [1] Upon cleavage, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify the activity of the β5i/LMP7 subunit of the 20S immunoproteasome. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively. Reference[1]. Winter, M.B., La Greca, F., Arastu-Kapur, S., et al. Immunoproteasome functions explained by divergence in cleavage specificity and regulation. ... | |||
T11924 |
M3258
LMP7-IN-1 |
Proteasome | Proteases/Proteasome; Ubiquitination |
LMP7-IN-1 may used in the research of inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer, is an inhibitor of immunoproteasome (LMP7). | |||
T15678 |
KZR-504
|
Proteasome | Proteases/Proteasome; Ubiquitination |
KZR-504 is a selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2) (IC50s: 51 nM, 4.274 μM for LMP2 and LMP7, respectively). | |||
T39653 |
Zetomipzomib maleate
Zetomipzomib maleate,KZR-616 maleate |
||
Zetomipzomib maleate (KZR-616), a novel immunoproteasome inhibitor, effectively and selectively inhibits the LMP7 subunit (hLMP7/mLMP7 IC50: 39/57 nM) and LMP2 subunit (hLMP7/mLMP7 IC50: 131/179 nM) of the immunoproteasome. This compound shows promising potential for research in various autoimmune diseases. | |||
T37419 | Zetomipzomib | ||
KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhib... | |||
T73986 | ONX-0914 TFA | ||
ONX-0914 (PR-957) TFA 为针对免疫蛋白酶体中的LMP7(低分子量多肽-7)的选择性抑制剂,LMP7为类糜蛋白酶亚单位。该化合物通过抑制细胞因子产生,减缓实验性关节炎进展,并已证实为分枝杆菌蛋白酶体的非竞争性不可逆抑制剂(Ki=5.2 μM)。此外,ONX-0914 TFA 能通过HSF-1介导的p-TEFb活化,激活潜伏的HIV-1。 |