| MPAKA # | Dzina lazogulitsa | Kufotokozera |
| Chithunzi cha CPD100616 | Emricasan | Emricasan, yemwe amadziwikanso kuti IDN 6556 ndi PF 03491390, ndi yoyamba mu kalasi caspase inhibitor mu mayesero a zachipatala pofuna kuchiza matenda a chiwindi. Emricasan (IDN-6556) imachepetsa kuvulala kwa chiwindi ndi fibrosis mu chitsanzo cha murine cha steatohepatitis yopanda mowa. IDN6556 imathandizira kujambulidwa kwachisumbu chambiri mumtundu waporcine islet autotransplant. Oral IDN-6556 ikhoza kuchepetsa ntchito ya aminotransferase kwa odwala omwe ali ndi matenda a hepatitis C. PF-03491390 yogwiritsidwa ntchito pamlomo imasungidwa m'chiwindi kwa nthawi yaitali ndi mawonekedwe otsika kwambiri, omwe amachititsa hepatoprotective zotsatira motsutsana ndi kuwonongeka kwa chiwindi cha alpha-fas mu chitsanzo cha mbewa. . |
| Chithunzi cha CPD100615 | Q-VD-Oph | QVD-OPH, yomwe imadziwikanso kuti Quinoline-Val-Asp-Difluorophenoxymethylketone, ndi wide spectrum caspase inhibitor yokhala ndi antiapoptotic properties. Q-VD-OPh imalepheretsa kukwapula kwa mwana wakhanda mu makoswe a P7: gawo la jenda. Q-VD-OPh ili ndi zotsatira zotsutsana ndi khansa ya m'magazi ndipo imatha kuyanjana ndi ma analogi a vitamini D kuonjezera chizindikiro cha HPK1 m'maselo a AML. Q-VD-OPh imachepetsa apoptosis yopwetekedwa ndi kupwetekedwa mtima komanso imathandizira kubwezeretsanso ntchito ya mwendo wakumbuyo mu makoswe pambuyo pa kuvulala kwa msana. |
| Chithunzi cha CPD100614 | Z-DEVD-FMK | Z-DEVD-fmk ndi cell-permeable, yosasinthika inhibitor ya caspase-3. Caspase-3 ndi cysteineyl aspartate-specific protease yomwe imagwira ntchito yayikulu mu apoptosis. |
| CPD100613 | Z-IETD-FMK | MDK4982, yomwe imadziwikanso kuti Z-IETD-FMK, ndi yamphamvu, yopitikizidwa ndi cell, yosasinthika inhibitor ya caspase-8 ndi granzyme B., Caspase-8 Inhibitor II imayang'anira zochitika zamoyo za Caspase-8. MDK4982 imalepheretsa bwino apoptosis yoyambitsidwa ndi kachilombo ka fuluwenza m'maselo a HeLa. MDK4982 imalepheretsanso granzyme B. MDK4982 ili ndi CAS#210344-98-2. |
| CPD100612 | Z-VAD-FMK | Z-VAD-FMK ndi cell-permeable, yosasinthika pan-caspase inhibitor. Z-VAD-FMK imalepheretsa kukonza caspase ndi kulowetsedwa kwa apoptosis m'maselo otupa mu vitro (IC50 = 0.0015 - 5.8 mM). |
| CPD100611 | Belnacasan | Belnacasan, yomwe imadziwikanso kuti VX-765, idapangidwa kuti iziletsa Caspase, yomwe ndi puloteni yomwe imayendetsa kupanga ma cytokines awiri, IL-1b ndi IL-18. VX-765 yasonyezedwa kuti imaletsa kukomoka koopsa m'mafanizo a preclinical. Kuphatikiza apo, VX-765 yawonetsa zochitika mumitundu yoyambirira ya khunyu. VX-765 inali itayikidwa pa odwala oposa 100 mu mayesero a chipatala a gawo-I ndi gawo-IIa okhudzana ndi matenda ena, kuphatikizapo mayesero a chipatala a 28-day-IIa odwala psoriasis. Yatsiriza gawo la chithandizo cha gawo-IIa lachidziwitso chachipatala cha VX-765 chomwe chinalembetsa pafupifupi odwala 75 omwe ali ndi khunyu yosamva mankhwala. Mayesero achipatala akhungu, osasinthika, oyendetsedwa ndi placebo adapangidwa kuti ayese chitetezo, kulekerera ndi zochitika zachipatala za VX-765. |
| CPD100610 | Maraviroc | Maraviroc ndi antiviral, wamphamvu, wosapikisana ndi CKR-5 receptor antagonist yomwe imalepheretsa kumanga kwa HIV viral coat protein gp120. Maraviroc amaletsa MIP-1β-stimulated γ-S-GTP kumangiriza ku HEK-293 cell membranes, kusonyeza mphamvu yake yoletsa kukhudzidwa kwa chemokine-kudalira kwa GDP-GTP kusinthana pa CKR-5/G protein complex. Maraviroc imalepheretsanso zochitika zapansi pa chemokine-induced intracellular calcium redistribution. |
| CPD100609 | Resatorvid | Resatorvid, yomwe imadziwikanso kuti TAK-242, ndi cell-permeable inhibitor ya TLR4 signing, kutsekereza LPS-induced kupanga NO, TNF-α, IL-6, ndi IL-1β mu macrophages ndi IC50 values of 1-11 nM. Resatorvid imamanga mosankha ku TLR4 ndikusokoneza kulumikizana pakati pa TLR4 ndi ma adapter mamolekyu ake. Resatorvid imapereka neuroprotection pakuyesa kuvulala koopsa kwaubongo: tanthauzo pochiza kuvulala kwaubongo wamunthu |
| CPD100608 | ASK1-Inhibitor-10 | ASK1 Inhibitor 10 ndi orally bioavailable inhibitor ya apoptosis signal-regulating kinase 1 (ASK1). Imasankha ASK1 pa ASK2 komanso MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, ndi B-RAF. Imalepheretsa kuwonjezeka kwa streptozotocin-induced mu JNK ndi p38 phosphorylation mu INS-1 pancreatic β maselo m'njira yodalira ndende. |
| Chithunzi cha CPD100607 | K811 | K811 ndi ASK1-specific inhibitor yomwe imatalikitsa kupulumuka mu mtundu wa mbewa wa amyotrophic lateral sclerosis. K811 imalepheretsa bwino kuchulukana kwa maselo m'maselo okhala ndi mawu apamwamba a ASK1 komanso ma cell a HER2-overexpressing GC. Kuchiza ndi K811 kumachepetsa kukula kwa zotupa za xenograft pochepetsa zolembera za kuchuluka. |
| Chithunzi cha CPD100606 | K812 | K812 ndi ASK1-specific inhibitor yomwe yapezedwa kuti italikitse kupulumuka mu mtundu wa mbewa wa amyotrophic lateral sclerosis. |
| Chithunzi cha CPD100605 | MSC-2032964A | MSC 2032964A ndi yamphamvu komanso yosankha ASK1 inhibitor (IC50 = 93 nM). Imaletsa LPS-induced ASK1 ndi p38 phosphorylation mu astrocyte otukuka a mbewa ndikupondereza neuroinflammation mumtundu wa EAE wa mbewa. MSC 2032964A ndi bioavailable pakamwa komanso kulowa muubongo. |
| Chithunzi cha CPD100604 | Selonsertib | Selonsertib, yomwe imadziwikanso kuti GS-4997, ndi inhibitor yapakamwa ya bioavailable ya apoptosis sign-regulating kinase 1 (ASK1), yokhala ndi anti-yotupa, anti-antineoplastic komanso anti-fibrotic. GS-4997 imayang'ana ndikumanga ku catalytic kinase domain ya ASK1 mumpikisano wa ATP, potero imalepheretsa phosphorylation ndi kutsegula kwake. GS-4997 imalepheretsa kupanga ma cytokines otupa, kutsika-kuwongolera mawonekedwe a majini omwe amakhudzidwa ndi fibrosis, kupondereza apoptosis kwambiri ndikuletsa kuchuluka kwa ma cell. |
| CPD100603 | Mtengo wa MDK36122 | MDK36122, yomwe imadziwikanso kuti H-PGDS Inhibitor I, ndi Prostaglandin D Synthase (hematopoietic-type) Inhibitor. MDK36122 ilibe code code, ndipo ili ndi CAS#1033836-12-2. Manambala 5 omaliza adagwiritsidwa ntchito kutchula dzina kuti azilumikizana mosavuta. MDK36122 imatsekereza HPGDS (IC50s = 0.7 ndi 32 nM mu ma enzyme ndi kuyesa kwa ma cell, motsatana) popanda kuchitapo kanthu motsutsana ndi ma enzymes aumunthu L-PGDS, mPGES, COX-1, COX-2, ndi 5-LOX. |
| CPD100602 | Tepoxalin | Tepoxalin, yomwe imadziwikanso kuti ORF-20485; RWJ-20485; ndi 5-lipoxygenase inhibitor yomwe ingathe kuchiza mphumu, osteoarthritis (OA). Tepoxalin ali mu vivo inhibitory ntchito motsutsana ndi COX-1, COX-2, ndi 5-LOX mwa agalu pa mlingo wovomerezeka wamakono. Tepoxalin imakulitsa ntchito ya antioxidant, pyrrolidine dithiocarbamate, pochepetsa tumor necrosis factor alpha-induced apoptosis mu WEHI 164 maselo. |
| CPD100601 | Tenidap | Tenidap, yemwe amadziwikanso kuti CP-66248, ndi COX/5-LOX inhibitor ndi cytokine-modulating anti-inflammatory drug candidate yomwe inali pansi pa Pfizer monga chithandizo chodalirika cha nyamakazi ya nyamakazi, koma Pfizer anaimitsa chitukuko pambuyo povomerezedwa ndi malonda. ndi FDA mu 1996 chifukwa cha chiwopsezo cha chiwindi ndi impso, chomwe chimatchedwa metabolites ya mankhwala okhala ndi thiophene moiety yomwe inayambitsa kuwonongeka kwa okosijeni. |
| CPD100600 | PF-4191834 | PF-4191834 ndi buku, lamphamvu komanso losankha lomwe si redox 5-lipoxygenase inhibitor lomwe limagwira ntchito pa kutupa ndi kupweteka. PF-4191834 imawonetsa potency yabwino mu ma enzyme- ndi ma cell-based assays, komanso mumtundu wa makoswe otupa kwambiri. Zotsatira za kuyesa kwa enzyme zikuwonetsa kuti PF-4191834 ndi inhibitor yamphamvu ya 5-LOX, yokhala ndi IC(50) = 229 +/- 20 nM. Kuphatikiza apo, idawonetsa pafupifupi 300-fold selectivity ya 5-LOX pa 12-LOX ndi 15-LOX ndipo ikuwonetsa palibe ntchito yokhudzana ndi michere ya cyclooxygenase. Kuonjezera apo, PF-4191834 imalepheretsa 5-LOX m'maselo a magazi a munthu, ndi IC (80) = 370 +/- 20 nM. |
| CPD100599 | Mtengo wa MK-886 | MK-886, yemwenso amadziwika kuti L 663536, ndi mdani wa leukotriene. Ikhoza kuchita izi poletsa 5-lipoxygenase activating protein (FLAP), motero imalepheretsa 5-lipoxygenase (5-LOX), ndipo ingathandize kuchiza atherosclerosis. MK-886 imalepheretsa ntchito ya cyclooxygenase-1 ndikupondereza kuphatikizika kwa mapulateleti. MK-886 imapangitsa kusintha kwa ma cell ndikuwonjezera apoptosis pambuyo pa photodynamic mankhwala ndi hypericin. MK-886 imapangitsa kusiyana kwa tumor necrosis factor-alpha-induced differentiation ndi apoptosis. |
| CPD100598 | L-691816 | L 691816 ndi inhibitor yamphamvu ya 5-LO reaction in vitro komanso mitundu ingapo yama vivo. |
| CPD100597 | CMI-977 | CMI-977, yomwe imadziwikanso kuti LPD-977 ndi MLN-977, ndi inhibitor yamphamvu ya 5-lipoxygenase yomwe imalowerera pakupanga ma leukotrienes ndipo pakali pano ikupangidwira kuchiza mphumu yosatha. CMI-977 imaletsa njira ya 5-lipoxygenase (5-LO) yotupa ma cell kuti itseke m'badwo wa leukotrienes, womwe umathandizira kwambiri pakuyambitsa mphumu ya bronchial. |
| CPD100596 | Mtengo wa CJ-13610 | CJ-13610 ndi choletsa pakamwa cha 5-lipoxygenase (5-LO) . CJ-13610 imalepheretsa biosynthesis ya leukotriene B4 ndikuwongolera IL-6 mRNA mawu mu macrophages. Ndiwothandiza mu zitsanzo zowawa za preclinical. |
| CPD100595 | BRP-7 | BRP-7 ndi 5-LO activating protein (FLAP) inhibitor. |
| CPD100594 | TT15 | TT15 ndi agonist wa GLP-1R. |
| CPD100593 | VU0453379 | VU0453379 ndi CNS-lolowera glucagon-ngati peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM) |
