| PUSI # | Igoa Oloa | Fa'amatalaga |
| CPD100616 | Emricasan | Emricasan, e lauiloa foi o le IDN 6556 ma le PF 03491390, o se fa'atosina caspase muamua-i-vasega i faʻataʻitaʻiga faʻapitoa mo togafitiga o faʻamaʻi ate. Emricasan (IDN-6556) faʻaitiitia le manua o le ate ma le fibrosis i se faʻataʻitaʻiga murine ole steatohepatitis e le o le ava malosi. IDN6556 fa'afaigofieina le fa'apipi'iina o tama'i motu tele i se fa'ata'ita'iga autotransplant tama'i puaa. Oral IDN-6556 e mafai ona faʻaitiitia ai le gaioiga aminotransferase i tagata mamaʻi e maua i le hepatitis C. O le tuʻuina atu o le PF-03491390 o loʻo taofia i totonu o le ate mo taimi uumi ma le maualalo o le faʻaogaina o le tino, faʻaaogaina se aafiaga hepatoprotective e faasaga i manuʻa ate alpha-fas i se faʻataʻitaʻiga isumu. . |
| CPD100615 | Q-VD-Oph | QVD-OPH, e taʻua foi o Quinoline-Val-Asp-Difluorophenoxymethylketone, o se faʻalavelave faʻapipiʻi caspase lautele faʻatasi ai ma mea malosi antiapoptotic. Q-VD-OPh e puipuia le ta'i o pepe pepe ile iole P7: ose matafaioi mo itupa. O le Q-VD-OPh e iai a'afiaga o le leukemia ma e mafai ona fegalegaleai ma vaitamini D analogs e fa'ateleina ai le fa'ailoga HPK1 i sela AML. Q-VD-OPh e faʻaitiitia ai le apoptosis faʻaleagaina ma faʻaleleia le toe faʻaleleia o le faʻaogaina o lima i isumu pe a maeʻa manua o le vaʻa. |
| CPD100614 | Z-DEVD-FMK | O le Z-DEVD-fmk o se masini e mafai ona faʻaogaina, e le mafai ona faʻaaogaina o le caspase-3. Caspase-3 o le cysteinyl aspartate-specific protease lea e faia se sao tutotonu i apoptosis. |
| CPD100613 | Z-IETD-FMK | MDK4982, lea e taʻua foi o le Z-IETD-FMK, o se mea malosi, cell-permeable, le mafai ona toe faʻafoʻiina o le caspase-8 ma le granzyme B., O le Caspase-8 Inhibitor II e pulea le gaioiga o meaola o Caspase-8. O le MDK4982 e taofia lelei le apoptosis e mafua mai i le siama i totonu o sela HeLa. MDK4982 fa'agata fo'i le granzyme B. MDK4982 iai CAS#210344-98-2. |
| CPD100612 | Z-VAD-FMK | O le Z-VAD-FMK o se masini e mafai ona faʻaogaina, e le mafai ona faʻaaogaina pan-caspase inhibitor. O le Z-VAD-FMK e taofia ai le faʻaogaina o le caspase ma le faʻaogaina o le apoptosis i sela tumo i vitro (IC50 = 0.0015 - 5.8 mM). |
| CPD100611 | Belnacasan | Belnacasan, lea e lauiloa foi o le VX-765, ua mamanuina e taofia Caspase, o se enzyme e pulea le gaosiga o lua cytokines, IL-1b ma IL-18. VX-765 ua faʻaalia e taofiofia le faoa faamalosi i faʻataʻitaʻiga faʻapitoa. E le gata i lea, VX-765 ua faʻaalia le gaioiga i faʻataʻitaʻiga faʻapitoa o le epilepsy masani. VX-765 na fa'aigoaina i le silia ma le 100 tagata gasegase i le vaega-I ma le vaega-IIa fa'ata'ita'iga fa'apitoa e feso'ota'i ma isi fa'ama'i, e aofia ai le 28-aso fa'ata'ita'iga-IIa fa'ata'ita'iga i tagata mama'i ma le psoriasis. Ua maeʻa le vaega o togafitiga o se vaega-IIa faʻataʻitaʻiga o le VX-765 lea na lesitalaina pe tusa ma le 75 tagata mamaʻi e maua i togafitiga epilepsy. O le faʻataʻitaʻiga faʻataʻitaʻi lua-tauaso, faʻafuaseʻi, placebo-pulea faʻataʻitaʻiga faʻataʻitaʻiga na fuafuaina e iloilo ai le saogalemu, faʻamalieina ma le gaioiga o le VX-765. |
| CPD100610 | Maraviroc | Maraviroc ose antiviral, malosi, le tauva CKR-5 antagonist talitali e taofia ai le fusifusia o le HIV viral coat protein gp120. Maraviroc faʻalavelaveina le MIP-1β-stimulated γ-S-GTP faʻapipiʻi i le HEK-293 cell membranes, e faʻaalia ai lona gafatia e faʻafefe ai le chemokine-faʻalagolago i le faʻaogaina o le GDP-GTP i le CKR-5 / G protein complex. Maraviroc e faʻalavelaveina foʻi le mea na tupu i lalo ole chemokine-induced intracellular calcium redistribution. |
| CPD100609 | Restatorvid | Resitorvid, lea e taʻua foi o TAK-242, o se inhibitor cell-permeable o le TLR4 faailoilo, poloka LPS-faʻaosoina le gaosiga o NO, TNF-α, IL-6, ma IL-1β i macrophages ma IC50 tau o 1-11 nM. Resatorvid e fusifusia filifilia i le TLR4 ma faʻalavelave i fegalegaleaiga i le va o le TLR4 ma ona mole faʻapipiʻi. Resitorvid e tuʻuina atu le neuroprotection i le faʻataʻitaʻiga manuʻa o le faiʻai: aʻafiaga i le togafitiga o manua o le faiʻai o le tagata |
| CPD100608 | ASK1-Inhibitor-10 | ASK1 Inhibitor 10 o se fa'agata fa'aola fa'aolaola ole apoptosis signal-regulating kinase 1 (ASK1). E filifilia mo ASK1 i luga ole ASK2 faʻapea foi MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, ma B-RAF. E taofia ai le faateleina o le streptozotocin i le JNK ma le p38 phosphorylation i le INS-1 pancreatic β sela i se tulaga faʻalagolago. |
| CPD100607 | K811 | K811 ose ASK1-specific inhibitor e faʻaumiina le ola i se faʻataʻitaʻiga o le isumu o le amyotrophic lateral sclerosis. O le K811 na puipuia lelei le fa'atuputeleina o sela i laina sela e maualuga le fa'aaliga ASK1 ma i le HER2-ova fa'amatalaga GC sela. Togafitiga fa'atasi ma K811 fa'aitiitia le lapopo'a o tuma xenograft e ala i le fa'alaloina o fa'ailoga fa'ateleina. |
| CPD100606 | K812 | K812 ose ASK1-specific inhibitor na maua e faʻaumi ai le ola i se faʻataʻitaʻiga o le isumu o le amyotrophic lateral sclerosis. |
| CPD100605 | MSC-2032964A | MSC 2032964A ose malosi ma filifili ASK1 inhibitor (IC50 = 93 nM). E poloka ai le LPS-induced ASK1 ma le p38 phosphorylation i astrocytes isumu aganuʻu ma taofia le neuroinflammation i se faʻataʻitaʻiga EAE kiore. MSC 2032964A o lo'o maua fa'aola fa'alaua'itele ma o'o i le fai'ai. |
| CPD100604 | Selonsertib | Selonsertib, lea e taʻua foi o le GS-4997, o se iniseti faʻaola e mafai ona faʻaogaina o le apoptosis signal-regulating kinase 1 (ASK1), faʻatasi ai ma gaioiga faʻamaʻi, antineoplastic ma anti-fibrotic. GS-4997 taulaʻi ma fusifusia i le catalytic kinase domain o le ASK1 i se ATP-faʻatauva, ma puipuia ai lona phosphorylation ma le faʻagaoioia. GS-4997 e taofia ai le gaosiga o cytokines inflammatory, lalo-faʻatonutonu le faʻaaliga o kenera e aʻafia i fibrosis, taofiofia le tele o apoptosis ma faʻalavelaveina le faʻalauteleina o le telefoni. |
| CPD100603 | MDK36122 | MDK36122, faʻapitoa foi o le H-PGDS Inhibitor I, o le Prostaglandin D Synthase (hematopoietic-type) Inhibitor. MDK36122 e leai se igoa fa'ailoga, ma e iai le CAS#1033836-12-2. O le numera 5 mulimuli na faʻaaogaina mo igoa mo fesoʻotaʻiga faigofie. MDK36122 filifili poloka HPGDS (IC50s = 0.7 ma 32 nM i enzyme ma cellular assays, faasologa) faʻatasi ai ma sina gaioiga e faʻatatau i enzymes tagata L-PGDS, mPGES, COX-1, COX-2, ma le 5-LOX. |
| CPD100602 | Tepoxalin | Tepoxalin, e lauiloa foi o le ORF-20485; RWJ-20485; ose 5-lipoxygenase inhibitor e mafai ona togafitia ai le sela, osteoarthritis (OA). Tepoxalin ei ai in vivo inhibitory gaoioiga e faasaga i COX-1, COX-2, ma le 5-LOX i maile i le taimi nei ua faamaonia fualaau fautuaina. Tepoxalin inhibits fula ma microvascular dysfunction faʻaosoina irradiation manava i isumu. Tepoxalin e faʻaleleia le gaioiga o se antioxidant, pyrrolidine dithiocarbamate, i le faʻaitiitia o le tumo necrosis factor alpha-induced apoptosis i WEHI 164 sela. |
| CPD100601 | Tenidap | Tenidap, lea e lauiloa foi o le CP-66248, o se COX/5-LOX inhibitor ma cytokine-modulating anti-inflammatory drug candidate lea sa i lalo o le atinaeina e le Pfizer e avea o se fuafuaga manuia togafitiga mo le gugu o le rheumatoid, ae na taofia e Pfizer le atinae ina ua teena le faamaoniga maketi. e le FDA i le 1996 ona o le ate ma fatugaʻo oona, lea na mafua mai i metabolites o le vailaʻau faʻatasi ma se vaega thiophene. na mafua ai le faaleagaina o le oxidative. |
| CPD100600 | PF-4191834 | PF-4191834 o se tala, malosi ma le filifilia e le redox 5-lipoxygenase inhibitor aoga i le mumū ma le tiga. O le PF-4191834 o loʻo faʻaalia ai le malosi lelei i suʻesuʻega faʻavae enzyme-ma sela, faʻapea foʻi ma se faʻataʻitaʻiga o le iole o le mumū ogaoga. Ole su'esu'ega ole enzyme e fa'aalia ai o le PF-4191834 ole malosi ole 5-LOX, ma le IC(50) = 229 +/- 20 nM. E le gata i lea, na faʻaalia pe tusa ma le 300-filifili filifiliga mo le 5-LOX i luga ole 12-LOX ma le 15-LOX ma faʻaalia e leai se gaioiga agai i le cyclooxygenase enzymes. E le gata i lea, o le PF-4191834 e taofia ai le 5-LOX i sela toto o le tagata, ma le IC(80) = 370 +/- 20 nM. |
| CPD100599 | MK-886 | MK-886, e taʻua foi o le L 663536, o le leukotriene antagonist. E mafai ona faia lenei mea e ala i le polokaina o le 5-lipoxygenase activating protein (FLAP), ma taofia ai le 5-lipoxygenase (5-LOX), ma e mafai ona fesoasoani i le togafitia o le atherosclerosis. O le MK-886 e taofia ai le gaioiga o le cyclooxygenase-1 ma taofia le faʻapipiʻiina o platelet. MK-886 faʻaosofia suiga i le taamilosaga o le cell ma faʻateleina apoptosis pe a maeʻa togafitiga photodynamic ma hypericin. MK-886 faʻaleleia le tumo necrosis factor-alpha-induced differentiation ma apoptosis. |
| CPD100598 | L-691816 | L 691816 ose fa'atosina malosi o le tali 5-LO e lua ile in vitro ma le tele o fa'ata'ita'iga in vivo. |
| CPD100597 | CMI-977 | CMI-977, ua lauiloa foi o le LPD-977 ma le MLN-977, o se inhibitor malosi 5-lipoxygenase e faʻalavelave i le gaosiga o leukotrienes ma o loʻo atiaʻe nei mo togafitiga o le fomaʻi masani. O le CMI-977 e taofia ai le 5-lipoxygenase (5-LO) cellular inflammation auala e poloka ai le gaosiga o leukotrienes, lea e faia se sao taua i le faʻaosoina o le sela bronchial. |
| CPD100596 | CJ-13610 | O le CJ-13610 o se fa'agata fa'amalosi tautala o le 5-lipoxygenase (5-LO) . CJ-13610 taofia le biosynthesis o leukotriene B4 ma faʻatonutonu le faʻamatalaga IL-6 mRNA i macrophages. E aoga i faʻataʻitaʻiga preclinical o tiga. |
| CPD100595 | BRP-7 | BRP-7 o le 5-LO activating protein (FLAP) inhibitor. |
| CPD100594 | TT15 | TT15 ole agonist ole GLP-1R. |
| CPD100593 | VU0453379 | VU0453379 o le CNS-penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM) |
