Caspase

CAT # Sunan samfur Bayani
Saukewa: CPD100616 Emricasan Emricasan, wanda kuma aka sani da IDN 6556 da PF 03491390, shine mai hanawar caspase na farko a cikin gwaji na asibiti don maganin cututtukan hanta. Emricasan (IDN-6556) yana rage raunin hanta da fibrosis a cikin samfurin murine na steatohepatitis mara giya. IDN6556 yana sauƙaƙa da haɓakar ɗimbin tsibiri a cikin ƙirar tsibiri autotransplant. IDN-6556 na baka na iya rage aikin aminotransferase a cikin marasa lafiya tare da ciwon hanta na kullum. PF-03491390 da aka sarrafa ta baki yana riƙe da hanta na tsawon lokaci tare da ƙananan bayyanar cututtuka, yana haifar da sakamako na hepatoprotective akan alpha-fas-induced hanta rauni a cikin wani linzamin kwamfuta model. .
Saukewa: CPD100615 Q-VD-Oph QVD-OPH, wanda kuma aka sani da Quinoline-Val-Asp-Difluorophenoxymethylketone, babban inhibitor caspase mai faɗi tare da kaddarorin antiapoptotic masu ƙarfi. Q-VD-OPh yana hana bugun jini na jariri a cikin P7 bera: rawar da jinsi. Q-VD-OPh yana da tasirin cutar sankarar bargo kuma yana iya hulɗa tare da analogs na bitamin D don haɓaka siginar HPK1 a cikin ƙwayoyin AML. Q-VD-OPh yana rage apoptosis da ke haifar da rauni kuma yana inganta dawo da aikin hind-gama a cikin berayen bayan rauni na kashin baya.
Saukewa: CPD100614 Z-DEVD-FMK Z-DEVD-fmk shine tantanin halitta, mai hanawa na caspase-3. Caspase-3 shine cysteinyl aspartate takamaiman protease wanda ke taka muhimmiyar rawa a cikin apoptosis.
Saukewa: CPD100613 Z-IETD-FMK MDK4982, wanda kuma aka sani da Z-IETD-FMK, mai ƙarfi ne, mai iya jurewa, mai hanawa na caspase-8 da granzyme B., Caspase-8 Inhibitor II yana sarrafa ayyukan nazarin halittu na Caspase-8. MDK4982 yadda ya kamata yana hana apoptosis mai haifar da mura a cikin ƙwayoyin HeLa. MDK4982 kuma yana hana granzyme B. MDK4982 yana da CAS # 210344-98-2.
Saukewa: CPD100612 Z-VAD-FMK Z-VAD-FMK mai iya jurewa tantanin halitta, mai hana pan-caspase wanda ba zai iya jurewa ba. Z-VAD-FMK yana hana aikin caspase da shigar da apoptosis a cikin ƙwayoyin tumor a cikin vitro (IC50 = 0.0015 - 5.8 mM).
Saukewa: CPD100611 Belnacasan Belnacasan, wanda aka fi sani da VX-765, an tsara shi don hana Caspase, wanda shine enzyme wanda ke kula da tsararrun cytokines guda biyu, IL-1b da IL-18. An nuna VX-765 don hana tsangwama a cikin ƙididdiga na asali. Bugu da kari, VX-765 ya nuna aiki a cikin preclinical model na kullum epilepsy. An yi amfani da VX-765 a cikin marasa lafiya fiye da 100 a cikin lokaci-I da na lokaci-IIa gwaji na asibiti da suka shafi wasu cututtuka, ciki har da gwajin gwaji na kwanaki 28-IIa a cikin marasa lafiya tare da psoriasis. Ya kammala lokacin jiyya na gwaji na asibiti na kashi-IIa na VX-765 wanda ya yi rajista kusan marasa lafiya 75 da farfadiya mai jure jiyya. An tsara gwajin makafi biyu, bazuwar, gwajin gwaji na asibiti don kimanta aminci, haƙuri da aikin asibiti na VX-765.
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