| IKATI # | Igama Lomkhiqizo | Incazelo |
| I-CPD100654 | Idatha ye-PD-169316 | I-PD-169316 iyisivimbeli esikhethiwe se-p38 MAPK. Ivimbela i-p38 MAPK nge-IC50 yama-89 nM. I-PD169316, ivimbela ukuguqulwa kwesici sokukhula kwe-beta-induced Smad kumaseli omdlavuza we-ovarian womuntu. |
| I-CPD100653 | I-LDN-193189 | I-LDN193189 iyi-molecule encane enamandla kakhulu ye-BMP inhibitor ene-IC50 ye-5 kanye ne-30 nM ye-ALK2 ne-ALK3, ngokulandelanayo. I-LDN193189 iphinde ivimbele uhlobo lwe-BMP I-receptors ALK6 (TGFβ1/BMP ukusayina) kanye ne-phosphorylation ye-SMAD elandelayo. |
| I-CPD100652 | K02288 | I-K02288 iyisivimbeli esinamandla sokusayina kwe-BMP. I-K02288 inomsebenzi we-in vitro ngokumelene ne-ALK2 ekugxilweni okuphansi kwe-nanomolar okufana nenhlanganisela yamanje yokuhola i-LDN-193189. I-K02288 ivimbele ngokuqondile indlela ye-BMP-induced Smad ngaphandle kokuthinta ukusayinda kwe-TGF-β kanye nokudonswa kwe-dorsalization ye-zebrafish embryos. |
| I-CPD100650 | I-SB-431542 | I-SB-431542 iyinoveli inhibitor encane ye-molecule yohlobo lwe-I TGF-beta receptor, kuphaneli yemigqa yeseli ye-glioma eyingozi. I-SB-431542 ivimbe i-phosphorylation kanye nokudluliselwa kwe-nuclear kwama-SMAD, abaxhumanisi be-intracellular bokusayina kwe-TGF-beta, ngokuloba okuncishisiwe kwe-TGF-beta-mediated. Ngaphezu kwalokho, i-SB-431542 ivimbele ukuvezwa kwemiphumela emibili ebalulekile ye-TGF-beta-vascular endothelial growth factor kanye ne-plasminogen activator inhibitor-1. |
| I-CPD100649 | GW788388 | I-GW788388 iyi-TGF-beta entsha yohlobo lwe-I receptor inhibitor enephrofayili ye-pharmacokinetic ethuthuke kakhulu uma iqhathaniswa ne-SB431542. Sifunde umphumela wayo ku-vitro futhi sathola ukuthi ivimbele kokubili uhlobo lwe-TGF-beta I kanye nemisebenzi yohlobo lwe-II ye-receptor kinase, kodwa hhayi leyo ye-bone morphogenic protein type II receptor. Ngaphezu kwalokho, ivimbele ukwenziwa kusebenze kwe-TGF-beta-induced Smad kanye nesisho sofuzo esiqondiwe, kuyilapho yehlisa ukuguquguquka kwe-epithelial-mesenchymal kanye ne-fibrogenesis. |
| I-CPD100648 | SB-525334 | I-SB525334 iyi-inhibitor enamandla futhi ekhethayo ye-transforming growth factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). I-SB525334 ivimbe umsebenzi we-ALK5 kinase nge-IC(50) ye-14.3 nM futhi yayinamandla angaphansi ngokuphindwe ka-4 njengesivimbeli se-ALK4 (IC(50) = 58.5 nM). I-SB-525334 ibingasebenzi njengesivimbeli se-ALK2, ALK3, ne-ALK6 (IC(50) > 10,000 nM). Ekuhlolweni okusekelwe kumaseli, i-SB-525334 (1 microM) ivimbe i-phosphorylation eyenziwe ye-TGF-beta1 kanye nokudluliselwa kwe-nuclear kwe-Smad2/3 kumaseli e-renal proximal tubule kanye nokwenyuka okuvinjiwe kwe-TGF-beta1 ku-plasminogen activator inhibitor-1 (PAI-1) ) kanye ne-procollagen alpha1(I) inkulumo ye-mRNA kumaseli e-A498 renal epithelial carcinoma. |
| I-CPD100647 | BIBF0775 | I-BIBF0775 iyisivimbeli sesici sokukhula esiguqukayo i-β receptor I (TGFβRI). Ukuhlaziywa kwesakhiwo se-X-ray kubonise ukuthi i-BIBF0775 ingene esizindeni se-kinase se-TGFβRI |
| I-CPD100646 | I-LY3023414 | I-LY3023414 i-molecule encane ekhonjiswe ku-vitro njenge-ATP-competitive inhibitor ekhethiwe ye-PI3Kα ne-mTOR, i-DNA-PK, namanye amalungu omndeni wesigaba I-PI3K. I-In vitro, i-LY3023414 ibonise umsebenzi wokuvimbela ngokumelene ne-PI3K ne-mTOR kumaseli we-tumor, kanye nomsebenzi wokulwa nokuvuvukala kanye nemiphumela yomjikelezo wamaseli. Ngaphezu kwalokho, ku-vitro, i-LY3023414 ivimbela ikhono le-PI3K ne-mTOR kuma-substrates e-phosphorylate endleleni ye-PI3K/mTOR. I-LY3023414 iyaphenywa ocwaningweni lomtholampilo lwesigaba I. |
| I-CPD100645 | I-Onatasertib | I-CC-223 iyi-inhibitor etholakala ngomlomo yethagethi ye-mammalian ye-rapamycin (mTOR) enekhono lomsebenzi we-antineoplastic. I-mTOR kinase inhibitor CC-223 ivimbela umsebenzi we-mTOR, okungase kuphumele ekungenisweni kwe-apoptosis yeseli yesimila kanye nokuncipha kokusabalala kweseli yesimila. I-mTOR, i-serine/threonine kinase elawulwa ezinhlobonhlobo zamathumba, idlala indima ebalulekile ezansi nomfula endleleni yokusayina ye-PI3K/AKT/mTOR, evamise ukulawulwa umdlavuza wabantu. |
| I-CPD100644 | Bimiralisib | I-Bimiralisib, eyaziwa nangokuthi i-PQR309, iyi-pan inhibitor etholakala ngomlomo ye-phosphoinositide-3-kinases (PI3K) kanye ne-inhibitor yethagethi ye-mammalian ye-rapamycin (mTOR), enekhono lomsebenzi we-antineoplastic. I-PI3K/mTOR kinase inhibitor PQR309 ivimbela i-PI3K kinase isoforms i-alpha, i-beta, i-gamma ne-delta futhi, ngezinga elincane, i-mTOR kinase, okungase kubangele i-tumor cell apoptosis kanye nokuvimbela ukukhula kumaseli aveza i-PI3K/mTOR ngokweqile. Ukwenza kusebenze indlela ye-PI3K/mTOR kukhuthaza ukukhula kwamaseli, ukusinda, nokumelana nakho kokubili ukwelashwa ngamakhemikhali kanye ne-radiotherapy. |
| I-CPD100643 | CZ415 | I-CZ415 iyi-mTOR inhibitor enamandla yokuncintisana ye-ATP enokukhethwa okungakaze kubonwe ngaphezu kwanoma iyiphi enye i-kinase (IC50 = 14.5 nM IC50 ye-pS6RP kanye ne-14.8 nM ye-pAKT) enokungena kweseli okuhle kakhulu (uhlelo lokusebenza lwe-Kd = 6.9 nM). Izakhiwo ze-Pharmacokinetic zokuvunyelwa okusesilinganisweni kanye ne-bioavailability enhle yomlomo ibonise ukufaneleka kwe-CZ415 yokuqhubekela phambili ezifundweni ze-vivo. I-CZ415 imele i-molecule efanelekile yophenyo lwemithi yendima ye-mTOR ye-pathophysiological ku-vivo. |
| I-CPD100642 | I-GDC-0084 | I-GDC-0084, eyaziwa nangokuthi i-RG7666 ne-Paxalisib, iyisivimbeli se-phosphatidylinositol 3-kinase (PI3K) esinomsebenzi we-antineoplastic ongaba khona. I-PI3K inhibitor GDC-0084 ivimbela ngokuqondile i-PI3K endleleni yokusayina ye-PI3K/AKT kinase (noma i-protein kinase B), ngaleyo ndlela ivimbele ukwenziwa kusebenze kwendlela yokusayina ye-PI3K. Lokhu kungase kuphumele ekuvinjweni kwakho kokubili ukukhula kwamangqamuzana nokuphila kumaseli e-tumor asengozini. Ukwenza kusebenze indlela yokusayina ye-PI3K kuvame ukuhlotshaniswa ne-tumorigenesis. |
| I-CPD100641 | I-CC-115 | I-CC-115 iyi-dual inhibitor ye-DNA-dependent protein kinase (DNA-PK) kanye nethagethi yezilwane ezincelisayo ye-rapamycin (mTOR), enomsebenzi ongaba khona we-antineoplastic. I-CC-115 ibophezela futhi ivimbele umsebenzi we-DNA-PK kanye nakho kokubili i-raptor-mTOR (i-TOR complex 1 noma i-TORC1) kanye ne-rictor-mTOR (i-TOR complex 2 noma i-TORC2), okungase kuholele ekunciphiseni ukwanda kwamaseli omdlavuza avezayo. I-DNA-PK ne-TOR. I-DNA-PK, i-serine/threonine kinase kanye nelungu lomndeni omncane ohlobene ne-PI3K we-kinase we-protein kinases, yenziwa yasebenza emonakalweni we-DNA futhi idlala indima ebalulekile ekulungiseni ukuphuka kwe-DNA enemicu kabili ngendlela ye-DNA nonnhomologous end joining (NHEJ) . |
| I-CPD100640 | XL388 | I-XL388 Ikilasi Lenoveli Elinamandla Kakhulu, Elikhethiwe, I-ATP-Competitive, kanye ne-Olly Bioavailable Inhibitors ye-Mammalian Target ye-Rapamycin (mTOR). I-XL388 ivimbele i-phosphorylation yeselula ye-mTOR complex 1 (p-p70S6K, pS6, ne-p-4E-BP1) kanye nama-substrates e-mTOR complex 2 (pAKT (S473)). I-XL388 ibonise i-pharmacokinetics enhle kanye nokuchayeka komlomo ezinhlotsheni eziningi ezine-bioavailability emaphakathi. Ukulawulwa komlomo kwe-XL388 kuya kumagundane anqunu e-athymic afakwe nge-xenograft yesimila somuntu kunikeze umsebenzi wokulwa nesimila obalulekile futhi oncike kumthamo. |
| I-CPD100639 | I-GDC-0349 | I-GDC-0349 iyingqamuzana elincane lesidakamizwa se-anticaner, elithuthukiswa yi-Genentech. Kusukela ngoJulayi 2012, i-Genentech ifake ukuhlolwa kwesigaba I se-GDC-0349 ukuze kuhlolwe Ukuphepha Nokubekezelelana kwe-GDC-0349 Ezigulini Ezinezimila Ezithuthukile Zasendaweni noma Ezine-Metastatic Solid noma i-Non Hodgkin's Lymphoma. |
| I-CPD100638 | I-ETP-46464 | I-ETP46464 iyisivimbeli se-DNA damage response response kinase Ataxia-telangiectasia mutated (ATM)- and Rad3-related (ATR). |
| I-CPD100637 | INDLELA-600 | I-WAY-600 iyisivimbeli esinamandla, esikwazi ukuncintisana ne-ATP futhi esikhethiwe se-mTOR ene-IC50 ye-9 nM |
| I-CPD100636 | I-WYE-687 | I-WYE-687 iyisivimbeli esinamandla futhi esiqhudelana ne-ATP futhi esikhethiwe se-mTOR ene-IC50 ye-7 nM. |
| I-CPD100635 | I-Palomid-529 | I-Palomid 529, eyaziwa nangokuthi i-P529, iyinoveli ye-PI3K/Akt/mTOR inhibitor. I-Palomid 529 (P529) ivimbela izakhiwo ze-TORC1 kanye ne-TORC2 futhi ibonisa kokubili ukuvimbela kokusayina kwe-Akt kanye nokusayina kwe-mTOR ngokufanayo kusimila nemithambo yegazi. Kwaboniswa ukuthi i-P529 ivimbele ukukhula kwesimila, i-angiogenesis, nokuqina kwemithambo. Igcine izici ezizuzisayo ze-tumor vascular normalization i-rapamycin eziqhayisa ngayo. Kodwa-ke, i-P529 ibonise inzuzo eyengeziwe yokuvimbela ukusayinda kwe-pAktS473 okuhambisana nokuvimbela i-TORC2 kuwo wonke amaseli futhi ngaleyo ndlela kudlule amaluphu empendulo aholela ekunyukeni kokusayina kwe-Akt kwamanye amaseli wesimila. (Umthombo: Cancer Res 008;68(22):9551?–7). |
| I-CPD100634 | I-BGT226-maleate | I-BGT226 iyisivimbeli se-phosphatidylinositol 3-kinase (PI3K) esinomsebenzi ongaba khona we-antineoplastic. I-PI3K inhibitor BGT226 ivimbela ngokuqondile i-PIK3 kumzila wokusayina we-PI3K/AKT kinase (noma i-protein kinase B), engase iqalise ukudluliselwa kwe-cytosolic Bax kulwelwesi olungaphandle lwe-mitochondrial, okwandisa ukukwazi ukungena kulwelwesi lwe-mitochondrial; Ukufa kwe-apoptotic cell kungase kulandele. U-Bax uyilungu lomndeni we-proapoptotic Bcl2 wamaprotheni. |
| I-CPD100633 | I-WYE-125132 | I-WYE-125132, eyaziwa nangokuthi i-WYE-132, inamandla kakhulu, i-ATP-nokuncintisana, futhi i-mTOR kinase inhibitor ethize (IC(50): 0.19 +/- 0.07 nmol/L; >5,000-fold selective against PI3Ks). I-WYE-132 ivimbele i-mTORC1 ne-mTORC2 kumamodeli ahlukahlukene omdlavuza ku-vitro kanye ne-vivo. Okubalulekile, okuhambisana nokukhishwa kofuzo kwe-mTORC2, i-WYE-132 ehlosiwe ye-P-AKT(S473) kanye nomsebenzi we-AKT ngaphandle kokunciphisa kakhulu izinga lokuzinza lomsebenzi we-PI3K/PDK1 we-biomarker P-AKT(T308), egqamisa isimiso esivelele nesiqondile. ye-AKT nge-mTORC2 kumaseli omdlavuza. |
| I-CPD100632 | I-Vistusertib | I-Vistusertib, eyaziwa nangokuthi i-AZD2014, iyisivimbeli esitholakala ngomlomo se-mammalian target of rapamycin (mTOR) esinokusebenza kwe-antineoplastic. I-mTOR kinase inhibitor AZD2014 ivimbela umsebenzi we-mTOR, okungase kuphumele ekuqalisweni kwe-tumor cell apoptosis kanye nokuncipha kokusabalala kweseli yesimila. I-mTOR, i-serine/threonine kinase elawulwa ngamathumba ahlukahlukene, idlala indima ebalulekile ezansi nomfula kumzila wokusayina we-PI3K/Akt/mTOR. |
| I-CPD100631 | I-WYE-354 | I-WYE-354 iyi-cell-permeable inhibitor enamandla ye-mTOR (IC50 = 4.3 nM) evimba ukusayina kukho kokubili i-mTOR complex 1 (mTORC1) ne-mTORC2. |
| I-CPD100630 | I-Gedatolisib | I-Gedatolisib, eyaziwa nangokuthi i-PKI-587 kanye ne-PF-05212384, i-ejenti eqondise i-phosphatidylinositol 3 kinase (PI3K) kanye nethagethi yezilwane ezincelisayo ye-rapamycin (mTOR) endleleni yokusayina ye-PI3K/mTOR, enekhono lomsebenzi we-antineoplastic. Lapho uphathwa nge-intravenous, i-PI3K/mTOR kinase inhibitor PKI-587 ivimbela kokubili i-PI3K kanye ne-mTOR kinases, okungase kubangele i-apoptosis kanye nokuvinjelwa kokukhula kwamangqamuzana omdlavuza ngokweqile kwe-PI3K/mTOR. Ukusebenza kwendlela ye-PI3K/mTOR kukhuthaza ukukhula kwamaseli, ukusinda, nokumelana nokwelashwa ngamakhemikhali kanye ne-radiotherapy; I-mTOR, i-serine/threonine kinase ezansi nomfula we-PI3K, ingase futhi yenziwe isebenze ngaphandle kwe-PI3K. |
