| CAT # | Khoom npe | Kev piav qhia |
| PIB 100616 | Emricasan | Emricasan, tseem hu ua IDN 6556 thiab PF 03491390, yog thawj-hauv-chav caspase inhibitor hauv kev sim tshuaj rau kev kho mob siab. Emricasan (IDN-6556) txo lub siab raug mob thiab fibrosis nyob rau hauv ib tug murine qauv ntawm non-alcoholic steatohepatitis. IDN6556 ua kom yooj yim marginal loj islet engraftment nyob rau hauv ib tug porcine islet autotransplant qauv. Qhov ncauj IDN-6556 tuaj yeem txo qis aminotransferase kev ua haujlwm hauv cov neeg mob uas muaj kab mob siab C. Orally-administered PF-03491390 yog khaws cia hauv daim siab rau lub sijhawm ntev nrog kev ua haujlwm tsis zoo, ua rau muaj kev tiv thaiv hepatoprotective tiv thaiv alpha-fas-induced daim siab raug mob hauv tus qauv nas. . |
| PIB 100615 | Q-VD-Oph | QVD-OPH, tseem hu ua Quinoline-Val-Asp-Difluorophenoxymethylketone, yog ib qho broad spectrum caspase inhibitor nrog muaj zog antiapoptotic zog. Q-VD-OPh tiv thaiv kev mob stroke hauv menyuam yaus hauv P7 nas: lub luag haujlwm rau poj niam txiv neej. Q-VD-OPh muaj kev tiv thaiv kab mob leukemia thiab tuaj yeem cuam tshuam nrog cov tshuaj vitamin D kom nce HPK1 signaling hauv AML hlwb. Q-VD-OPh txo cov kev raug mob vim raug apoptosis thiab txhim kho kev rov qab los ntawm hind-limb muaj nuj nqi hauv cov nas tom qab raug mob qaum. |
| PIB 100614 | Z-DEVD-FMK | Z-DEVD-fmk yog cell-permeable, irreversible inhibitor ntawm caspase-3. Caspase-3 yog cysteyl aspartate-specific protease uas ua lub luag haujlwm tseem ceeb hauv apoptosis. |
| PIB 100613 | Z-IETD-FMK | MDK4982, tseem hu ua Z-IETD-FMK, yog ib qho muaj zog, cell-permeable, irreversible inhibitor ntawm caspase-8 thiab granzyme B., Caspase-8 Inhibitor II tswj cov kev ua si lom neeg ntawm Caspase-8. MDK4982 muaj txiaj ntsig zoo inhibits tus kab mob khaub thuas-induced apoptosis hauv HeLa hlwb. MDK4982 kuj inhibits granzyme B. MDK4982 muaj CAS#210344-98-2. |
| PIB 100612 | Z-VAD-FMK | Z-VAD-FMK yog cell-permeable, irreversible pan-caspase inhibitor. Z-VAD-FMK inhibits caspase ua thiab apoptosis induction hauv qog hlwb hauv vitro (IC50 = 0.0015 - 5.8 mM). |
| PIB 100611 | Belnacasan | Belnacasan, tseem hu ua VX-765, yog tsim los inhibit Caspase, uas yog ib qho enzyme uas tswj cov tiam ntawm ob cytokines, IL-1b thiab IL-18. VX-765 tau pom tias inhibit mob qaug dab peg hauv cov qauv ua ntej. Tsis tas li ntawd, VX-765 tau qhia txog kev ua haujlwm hauv preclinical qauv ntawm kev mob vwm. VX-765 tau muab tshuaj rau ntau tshaj 100 tus neeg mob nyob rau theem-I thiab theem-IIa kev sim tshuaj ntsuam xyuas ntsig txog lwm yam kab mob, suav nrog 28-hnub theem-IIa kev sim tshuaj rau cov neeg mob psoriasis. Nws tau ua tiav cov theem kev kho mob ntawm theem-IIa kev sim tshuaj ntsuam xyuas ntawm VX-765 uas tau tso npe kwv yees li 75 tus neeg mob uas muaj kev tiv thaiv kab mob vwm. Qhov ob-dig muag, randomized, cov tshuaj placebo-tswj tshuaj ntsuam xyuas tau tsim los ntsuas kev nyab xeeb, kev ua siab ntev thiab kev kho mob ntawm VX-765. |
| PIB 100610 | Maraviroc | Maraviroc yog ib qho tshuaj tiv thaiv kab mob, muaj zog, tsis sib tw CKR-5 receptor antagonist uas inhibits kev khi ntawm HIV kab mob khaub ncaws protein gp120. Maraviroc inhibits MIP-1β-stimulated γ-S-GTP khi rau HEK-293 cell membranes, qhia nws lub peev xwm los inhibit chemokine-dependent stimulation ntawm GDP-GTP pauv ntawm CKR-5 / G protein complex. Maraviroc kuj inhibits qhov kev tshwm sim hauv qab ntawm chemokine-induced intracellular calcium redistribution. |
| PIB 100609 | Resatorvid | Resatorvid, tseem hu ua TAK-242, yog cell-permeable inhibitor ntawm TLR4 signaling, thaiv LPS-induced zus tau tej cov NO, TNF-α, IL-6, thiab IL-1β hauv macrophages nrog IC50 qhov tseem ceeb ntawm 1-11 nM. Resatorvid khi xaiv rau TLR4 thiab cuam tshuam nrog kev sib cuam tshuam ntawm TLR4 thiab nws cov khoom siv hloov pauv. Resatorvid muab kev tiv thaiv neuroprotection hauv kev sim ua rau lub hlwb raug mob: cuam tshuam hauv kev kho mob ntawm tib neeg lub hlwb raug mob |
| PIB 100608 | ASK1-Inhibitor-10 | ASK1 Inhibitor 10 yog qhov ncauj bioavailable inhibitor ntawm apoptosis signal-regulating kinase 1 (ASK1). Nws yog xaiv rau ASK1 tshaj ASK2 nrog rau MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, thiab B-RAF. Nws inhibits streptozotocin-induced nce nyob rau hauv JNK thiab p38 phosphorylation hauv INS-1 pancreatic β hlwb nyob rau hauv ib tug concentration-dependent yam. |
| PAB 100607 | k811 ua | K811 yog ASK1 tshwj xeeb inhibitor uas ua rau muaj sia nyob ntev hauv tus qauv nas ntawm amyotrophic lateral sclerosis. K811 ua tau zoo tiv thaiv cell proliferation hauv cov kab ntawm tes nrog siab ASK1 qhia thiab hauv HER2-overexpressing GC hlwb. Kev kho mob nrog K811 txo qhov ntau thiab tsawg ntawm xenograft hlav los ntawm kev txo qis cov cim kev loj hlob. |
| PIB 100606 | k812 ua | K812 yog ib qho ASK1 tshwj xeeb inhibitor tshawb pom kom muaj sia nyob ntev hauv tus qauv nas ntawm amyotrophic lateral sclerosis. |
| PIB 100605 | MSC-2032964A | MSC 2032964A yog lub zog thiab xaiv ASK1 inhibitor (IC50 = 93 nM). Nws thaiv LPS-induced ASK1 thiab p38 phosphorylation hauv kab lis kev cai nas astrocytes thiab suppresses neuroinflamation hauv tus nas EAE qauv. MSC 2032964A yog qhov ncauj bioavailable thiab lub hlwb nkag mus. |
| PIB 100604 | Selonsertib | Selonsertib, tseem hu ua GS-4997, yog ib qho kev hais lus bioavailable inhibitor ntawm apoptosis signal-regulating kinase 1 (ASK1), muaj peev xwm tiv thaiv kab mob, antineoplastic thiab anti-fibrotic kev ua ub no. GS-4997 lub hom phiaj thiab khi rau catalytic kinase domain ntawm ASK1 hauv kev sib tw ATP, yog li tiv thaiv nws cov phosphorylation thiab ua kom muaj zog. GS-4997 tiv thaiv kev tsim cov cytokines inflammatory, down-regulates cov kev qhia ntawm cov noob koom nrog fibrosis, suppresses ntau apoptosis thiab inhibits cellular proliferation. |
| PIB 100603 | TIAB SA 36122 | MDK36122, tseem hu ua H-PGDS Inhibitor I, yog Prostaglandin D Synthase (hematopoietic-type) Inhibitor. MDK36122 tsis muaj npe, thiab muaj CAS # 1033836-12-2. Tus lej 5 kawg tau siv rau lub npe rau kev sib txuas lus yooj yim. MDK36122 xaiv blocks HPGDS (IC50s = 0.7 thiab 32 nM hauv enzyme thiab cellular assays, ntsig txog) nrog kev ua haujlwm me me tawm tsam tib neeg cov enzymes L-PGDS, mPGES, COX-1, COX-2, thiab 5-LOX. |
| PIB 100602 | Tepoxalin | Tepoxalin, tseem hu ua ORF-20485; RWJ-20485; yog 5-lipoxygenase inhibitor muaj peev xwm kho mob hawb pob, osteoarthritis (OA). Tepoxalin muaj nyob rau hauv vivo inhibitory kev ua ub no tiv thaiv COX-1, COX-2, thiab 5-LOX hauv cov dev ntawm qhov kev pom zoo tam sim no noj. Tepoxalin txhim kho kev ua haujlwm ntawm cov tshuaj tua kab mob antioxidant, pyrrolidine dithiocarbamate, hauv kev txo qis qog necrosis yam alpha-induced apoptosis hauv WEHI 164 hlwb. |
| PIB 100601 | Tenidap | Tenidap, tseem hu ua CP-66248, yog COX / 5-LOX inhibitor thiab cytokine-modulating anti-inflammatory tus neeg sib tw uas tab tom txhim kho los ntawm Pfizer raws li kev cog lus muaj peev xwm kho mob rheumatoid mob caj dab, tab sis Pfizer nres kev txhim kho tom qab kev pom zoo kev lag luam raug tsis lees paub. los ntawm FDA nyob rau hauv 1996 vim lub siab thiab lub raum toxicity, uas yog ntaus nqi rau metabolites ntawm cov tshuaj nrog thiophene moiety uas ua rau oxidative puas tsuaj. |
| PIB 100600 | PF-4191834 | PF-4191834 yog ib qho tshiab, muaj zog thiab xaiv tsis-redox 5-lipoxygenase inhibitor zoo hauv kev mob thiab mob. PF-4191834 nthuav tawm lub zog zoo hauv enzyme- thiab kev soj ntsuam ntawm tes, nrog rau hauv cov qauv nas ntawm tus mob mob. Enzyme assay cov txiaj ntsig qhia tias PF-4191834 yog lub zog 5-LOX inhibitor, nrog IC (50) = 229 +/- 20 nM. Tsis tas li ntawd, nws pom tau hais tias kwv yees li 300-fold selectivity rau 5-LOX tshaj 12-LOX thiab 15-LOX thiab qhia tias tsis muaj kev cuam tshuam rau cov enzymes cyclooxygenase. Tsis tas li ntawd, PF-4191834 inhibits 5-LOX hauv tib neeg cov ntshav, nrog IC (80) = 370 +/- 20 nM. |
| PAB 100599 | TSI-886 | MK-886, tseem hu ua L 663536, yog leukotriene antagonist. Nws tuaj yeem ua qhov no los ntawm kev thaiv cov 5-lipoxygenase activating protein (FLAP), yog li inhibiting 5-lipoxygenase (5-LOX), thiab tuaj yeem pab kho atherosclerosis. MK-886 inhibits cyclooxygenase-1 kev ua haujlwm thiab inhibits platelet aggregation. MK-886 induces kev hloov hauv lub voj voog ntawm tes thiab nce apoptosis tom qab photodynamic kho nrog hypericin. MK-886 txhim kho qog necrosis yam-alpha-induced sib txawv thiab apoptosis. |
| PAB 100598 | L-691816 | L 691816 yog ib qho muaj zog inhibitor ntawm 5-LO cov tshuaj tiv thaiv ob qho tib si hauv vitro thiab ntau yam hauv vivo qauv. |
| PAB 100597 | TSI-977 | CMI-977, tseem paub tias yog LPD-977 thiab MLN-977, yog lub zog 5-lipoxygenase inhibitor uas cuam tshuam rau kev tsim cov leukotrienes thiab tam sim no tau tsim los kho mob hawb pob. CMI-977 inhibits 5-lipoxygenase (5-LO) cellular o txoj hauv kev los thaiv cov tiam ntawm leukotrienes, uas ua lub luag haujlwm tseem ceeb hauv kev ua rau mob hawb pob bronchial. |
| PIB 100596 | CJ-13610 | CJ-13610 yog ib qho active inhibitor ntawm 5-lipoxygenase (5-LO). CJ-13610 inhibits biosynthesis ntawm leukotriene B4 thiab tswj IL-6 mRNA qhia hauv macrophages. Nws muaj txiaj ntsig zoo hauv cov qauv ua ntej ntawm qhov mob. |
| PAB 100595 | BRP-7 | BRP-7 yog 5-LO activating protein (FLAP) inhibitor. |
| PIB 100594 | TT15 | TT15 yog agonist ntawm GLP-1R. |
| PIB 100593 | wb 0453379 | VU0453379 yog CNS-penetrant glucagon-zoo li peptide 1 receptor (GLP-1R) zoo allosteric modulator (PAM) |
