Caspase

CAT # Igama lemveliso Inkcazo
CPD100616 Emricasan I-Emricasan, eyaziwa ngokuba yi-IDN 6556 kunye ne-PF 03491390, yiklasi yokuqala ye-caspase inhibitor kwiimvavanyo zekliniki zonyango lwezifo zesibindi. I-Emricasan (IDN-6556) inciphisa ukulimala kwesibindi kunye ne-fibrosis kwimodeli ye-murine ye-steatohepatitis engeyiyo utywala. I-IDN6556 iququzelela ukumiliselwa kwesiqithi esiselunxwemeni kwimodeli ye-porcine islet autotransplant. I-IDN-6556 yomlomo inokunciphisa umsebenzi we-aminotransferase kwizigulane ezine-hepatitis C engapheliyo. I-PF-03491390 elawulwa ngomlomo igcinwe kwisibindi ixesha elide kunye ne-systemic exposure ephantsi, eqhuba i-hepatoprotective effect kwi-alpha-fas-induced isibindi yokulimala kwimodeli yegundane. .
CPD100615 Q-VD-Oph I-QVD-OPH, eyaziwa ngokuba yi-Quinoline-Val-Asp-Difluorophenoxymethylketone, i-wide spectrum caspase inhibitor eneempawu ezinamandla ze-antiapoptotic. I-Q-VD-OPh ikhusela i-neonatal stroke kwi-P7 rat: indima yesini. I-Q-VD-OPh ineempembelelo ezichasene ne-leukemia kwaye inokusebenzisana ne-vitamin D analogs ukunyusa ukubonakaliswa kwe-HPK1 kwiiseli ze-AML. I-Q-VD-OPh inciphisa i-apoptosis eyenziwa yi-trauma kwaye iphucula ukubuyiswa komsebenzi we-back-hend kumagundane emva kokulimala kwentambo yomgogodla.
CPD100614 Z-DEVD-FMK I-Z-DEVD-fmk yi-cell-permeable, inhibitor engenakunqandwa ye-caspase-3. I-Caspase-3 yi-cysteineyl aspartate-specific protease edlala indima ephambili kwi-apoptosis.
CPD100613 Z-IETD-FMK I-MDK4982, eyaziwa ngokuba yi-Z-IETD-FMK, inamandla, i-cell-permeable, inhibitor engenakunqandwa ye-caspase-8 kunye ne-granzyme B., I-Caspase-8 Inhibitor II ilawula umsebenzi we-biological we-Caspase-8. I-MDK4982 inqanda ngokufanelekileyo i-apoptosis eyenziwa yintsholongwane yomkhuhlane kwiiseli ze-HeLa. I-MDK4982 iphinda inqanda i-granzyme B. MDK4982 ine-CAS # 210344-98-2.
CPD100612 Z-VAD-FMK I-Z-VAD-FMK yi-cell-permeable, i-pan-caspase inhibitor engenakuguqulwa. I-Z-VAD-FMK inqanda ukusetyenzwa kwe-caspase kunye nokungeniswa kwe-apoptosis kwiiseli ze-tumor in vitro (IC50 = 0.0015 - 5.8 mM).
CPD100611 Belnacasan I-Belnacasan, eyaziwa ngokuba yi-VX-765, yenzelwe ukuvimbela i-Caspase, eyi-enzyme elawula ukuveliswa kwee-cytokines ezimbini, i-IL-1b kunye ne-IL-18. I-VX-765 ibonakaliswe ukuba inqanda ukubanjwa okukrakra kwiimodeli zangaphambili. Ukongeza, i-VX-765 ibonise umsebenzi kwiimodeli ze-preclinical zesithuthwane esingapheliyo. I-VX-765 iye yajoliswa kwizigulane ezingaphezu kwe-100 kwi-phase-I kunye ne-phase-IIa yolingo lweklinikhi olunxulumene nezinye izifo, kubandakanywa ulingo lwezonyango lwe-28-day-IIa kwizigulane ezine-psoriasis. Igqibe isigaba sonyango lwesigaba-IIa solingo lwezonyango lwe-VX-765 olubhalise malunga nezigulane ezingama-75 ezinesithuthwane esinganyangekiyo kunyango. Ulingo lwekliniki oluyimfama oluphindwe kabini, olungahleliwe, olulawulwa yi-placebo lwenzelwe ukuvavanya ukhuseleko, ukunyamezela kunye nomsebenzi weklinikhi we-VX-765.

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