| CAT # | Igama lemveliso | Inkcazo |
| CPD100654 | PD-169316 | I-PD-169316 yi-inhibitor ekhethiweyo ye-p38 MAPK. Ithintela i-p38 MAPK nge-IC50 ye-89 nM. I-PD169316, inqanda ukuguquka kwemeko yokukhula kwe-beta-induced Smad signaling kwiiseli zomhlaza wesibeleko somntu. |
| CPD100653 | I-LDN-193189 | I-LDN193189 yi-molecule enamandla kakhulu i-BMP inhibitor ene-IC50 ye-5 kunye ne-30 nM ye-ALK2 kunye ne-ALK3, ngokulandelanayo. I-LDN193189 iphinda inqanda uhlobo lwe-BMP I-receptors ye-ALK6 (i-TGFβ1 / i-BMP yokubonisa) kunye ne-phosphorylation ye-SMAD elandelayo. |
| CPD100652 | K02288 | I-K02288 yi-inhibitor enamandla yokubonisa i-BMP. I-K02288 inomsebenzi we-vitro ngokuchasene ne-ALK2 kwiindawo eziphantsi ze-nanomolar ezifana nekhompawundi ekhokelayo yangoku ye-LDN-193189. I-K02288 ithintele ngokukodwa indlela ye-BMP-induced Smad ngaphandle kokuchaphazela ukubonakaliswa kwe-TGF-β kunye ne-dorsalization ye-zebrafish embryos. |
| CPD100650 | SB-431542 | I-SB-431542 yinoveli encinci ye-molecule inhibitor yohlobo lwe-I TGF-beta receptor, kwiphaneli yemigca yeseli ye-glioma eyingozi. I-SB-431542 ivalele i-phosphorylation kunye ne-nuclear translocation ye-SMADs, abalamli be-intracellular ye-TGF-beta yokubonisa, kunye nokunciphisa i-TGF-beta-mediated transcription. Ngaphezu koko, i-SB-431542 ivimbele ukubonakaliswa kwezinto ezimbini ezibalulekileyo ze-TGF-beta-vascular endothelial growth factor kunye ne-plasminogen activator inhibitor-1. |
| CPD100649 | GW788388 | I-GW788388 luhlobo olutsha lwe-TGF-beta ye-I receptor inhibitor eneprofayili ephuculwe kakhulu ye-pharmacokinetic xa kuthelekiswa ne-SB431542. Sifunde umphumo wayo kwi-vitro kwaye safumanisa ukuba inhibite zombini i-TGF-beta uhlobo lwe-I kunye nohlobo lwe-II ye-receptor kinase imisebenzi, kodwa kungekhona i-bone morphogenic protein type II receptor. Ngaphaya koko, iye yavala i-TGF-beta-induced Smad activation kunye ne-target gene expression, ngelixa inciphisa utshintsho lwe-epithelial-mesenchymal kunye ne-fibrogenesis. |
| CPD100648 | SB-525334 | I-SB525334 yi-inhibitor enamandla kwaye ekhethiweyo yokuguqula ukukhula kwe-beta1 (TGF-beta1) i-receptor, i-activin receptor-like kinase (ALK5). I-SB525334 ivimbele umsebenzi we-ALK5 kinase nge-IC(50) ye-14.3 nM kwaye yayimalunga ne-4-fold less potent as an inhibitor of ALK4 (IC(50) = 58.5 nM). I-SB-525334 yayingasebenzi njenge-inhibitor ye-ALK2, ALK3, kunye ne-ALK6 (IC(50)> 10,000 nM). Kwii-assays ezisekelwe kwiiseli, i-SB-525334 (i-1 microM) ivalwe i-TGF-beta1-induced phosphorylation kunye ne-nuclear translocation ye-Smad2 / 3 kwiiseli ze-renal proximal tubule kunye ne-inhibited TGF-beta1-induced ukwanda kwi-plasminogen activator inhibitor-1 (PAI-1) ) kunye neprocollagen alpha1 (I) intetho ye-mRNA kwiiseli ze-A498 ze-renal epithelial carcinoma. |
| CPD100647 | BIBF0775 | I-BIBF0775 yi-inhibitor ye-transforming growth factor β receptor I (TGFβRI). Uhlalutyo lwesakhiwo se-X-ray lubonise ukuba i-BIBF0775 ifakwe kwi-kinase domain ye-TGFβRI |
| CPD100646 | LY3023414 | I-LY3023414 i-molecule encinci eboniswe kwi-vitro ibe yi-ATP-competitive inhibitor ekhethiweyo ye-PI3Kα kunye ne-mTOR, i-DNA-PK, kunye nezinye iklasi I-PI3K amalungu entsapho. I-In vitro, i-LY3023414 ibonise umsebenzi wokuthintela ngokuchasene ne-PI3K kunye ne-mTOR kwiiseli ze-tumor, kunye nomsebenzi ochasayo kunye nemiphumo ye-cell cycle. Ukongeza, kwi-vitro, i-LY3023414 inqanda amandla e-PI3K kunye ne-mTOR kwi-phosphorylate substrates kwindlela ye-PI3K / mTOR. I-LY3023414 iphandwa kwisigaba soku-I solingo lwezonyango. |
| CPD100645 | Onatasertib | I-CC-223 yi-inhibitor efumaneka ngomlomo kwithagethi ye-mammalian ye-rapamycin (mTOR) enomsebenzi onokuthi ube ne-antineoplastic. I-mTOR kinase inhibitor CC-223 inqanda umsebenzi we-mTOR, onokuthi ubangele ukufakwa kwe-tumor cell apoptosis kunye nokuncipha kwe-tumor cell proliferation. I-mTOR, i-serine / i-threonine kinase elawulwa kwiindidi ezahlukeneyo ze-tumor, idlala indima ebalulekileyo ezantsi kwindlela yokubonisa i-PI3K / AKT / mTOR, ehlala i-dysregulated kwi-cancer yabantu. |
| CPD100644 | Bimiralisib | I-Bimiralisib, eyaziwa ngokuba yi-PQR309, i-pan inhibitor ye-bioavailable ngomlomo ye-phosphoinositide-3-kinases (PI3K) kunye ne-inhibitor ye-mammalian target of rapamycin (mTOR), enokuthi isebenze i-antineoplastic. I-PI3K/mTOR kinase inhibitor PQR309 inqanda i-PI3K kinase isoforms alpha, beta, gamma kunye ne-delta kwaye, kwinqanaba elingaphantsi, i-mTOR kinase, enokuthi ibangele i-tumor cell apoptosis kunye nokuvinjelwa kokukhula kwiiseli ezigqithise i-PI3K / mTOR. Ukusebenza kwendlela ye-PI3K / mTOR ikhuthaza ukukhula kweeseli, ukusinda, kunye nokuchasana ne-chemotherapy kunye ne-radiotherapy. |
| CPD100643 | CZ415 | I-CZ415 inamandla e-ATP-ekhuphisana ne-mTOR inhibitor ene-selectivity engazange ibonwe ngaphezu kwayo nayiphi na enye i-kinase (IC50 = 14.5 nM IC50 ye-pS6RP kunye ne-14.8 nM ye-pAKT) ene-cell permeability enhle kakhulu (Kd app = 6.9 nM). Iipropati ze-Pharmacokinetic zokukhutshwa okuphakathi kunye ne-bioavailability efanelekileyo yomlomo ibonise ukufaneleka kwe-CZ415 yokuqhubela phambili kwizifundo ze-vivo. I-CZ415 imele imolekyuli efanelekileyo yophando lwe-pharmacological ye-mTOR pathophysiological indima kwi-vivo. |
| CPD100642 | GDC-0084 | I-GDC-0084, eyaziwa ngokuba yi-RG7666 kunye ne-Paxalisib, i-phosphatidylinositol 3-kinase (PI3K) inhibitor enokuthi isebenze i-antineoplastic. I-PI3K inhibitor i-GDC-0084 inqanda ngokukodwa i-PI3K kwi-PI3K / AKT kinase (okanye iprotein kinase B) indlela yokubonisa, ngaloo ndlela inqanda ukusetyenziswa kwe-PI3K indlela yokubonisa. Oku kunokukhokelela ekuthinteleni kokubini ukukhula kweeseli kunye nokusinda kwi-cell tumor cell populations. Ukusebenza kwendlela yokubonisa i-PI3K ihlala ihambelana ne-tumorigenesis. |
| CPD100641 | CC-115 | I-CC-115 yi-inhibitor emibini ye-DNA-exhomekeke kwiprotheni kinase (DNA-PK) kunye nethagethi ye-mammalian ye-rapamycin (mTOR), kunye nomsebenzi onokuthi ube ne-antineoplastic. I-CC-115 ibophelela kwaye inqanda umsebenzi we-DNA-PK kunye zombini i-raptor-mTOR (i-TOR eyinkimbinkimbi 1 okanye i-TORC1) kunye ne-rictor-mTOR (i-TOR complex 2 okanye i-TORC2), enokuthi iholele ekunciphiseni ukwanda kweeseli zomhlaza ezivakalisa I-DNA-PK kunye neTOR. I-DNA-PK, i-serine / threonine kinase kunye nelungu le-PI3K-related kinase subfamily yeprotein kinases, isebenze kumonakalo we-DNA kwaye idlala indima ephambili ekulungiseni ukuphulwa kwe-DNA ephindwe kabini nge-DNA ye-nonhomologous end joining (NHEJ) indlela. . |
| CPD100640 | XL388 | I-XL388 yiKlasi yeNoveli yeNqanaba eliPhezulu, eliKhethekileyo, le-ATP-Competitive, kunye ne-Olly Bioavailable Inhibitors ye-Mammalian Target ye-Rapamycin (mTOR). I-XL388 inhibited phosphorylation yeselula ye-mTOR complex 1 (p-p70S6K, pS6, kunye ne-p-4E-BP1) kunye ne-mTOR complex 2 (pAKT (S473)) substrates. I-XL388 ibonise i-pharmacokinetics elungileyo kunye nokuvezwa komlomo kwiintlobo ezininzi kunye ne-bioavailability ephakathi. Ulawulo lomlomo lwe-XL388 ukuya kwiimpuku ze-athymic ze-athymic ezifakwe kwi-tumor xenografts yabantu zinike umsebenzi obalulekileyo kunye nokuxhomekeka kwidosi ye-antitumor. |
| CPD100639 | GDC-0349 | I-GDC-0349 yimolekyuli encinci ye-anticaner umgqatswa wamachiza, ephuhliswa yi-Genentech. Ukususela ngoJulayi ka-2012, i-Genentech iye yafaka ulingo lwesigaba soku-I se-GDC-0349 sokuvavanya uKhuseleko noNyamezelo lwe-GDC-0349 kwiZigulana ezinamaqhuma aPhakamileyo okanye aneMetastatic Solid okanye i-Non Hodgkin's Lymphoma. |
| CPD100638 | ETP-46464 | I-ETP46464 yi-inhibitor ye-DNA yokuphendula umonakalo we-kinase Ataxia-telangiectasia mutated (ATM)- kunye ne-Rad3-ehlobene (ATR). |
| CPD100637 | INDLELA-600 | I-WAY-600 inamandla, i-ATP-ekhuphisanayo kunye ne-inhibitor ekhethiweyo ye-mTOR ene-IC50 ye-9 nM |
| CPD100636 | WYE-687 | I-WYE-687 inamandla kunye ne-ATP-ekhuphisanayo kunye ne-inhibitor ekhethiweyo ye-mTOR kunye ne-IC50 ye-7 nM. |
| CPD100635 | Palomid-529 | I-Palomid 529, eyaziwa ngokuba yi-P529, yinoveli ye-PI3K/Akt/mTOR inhibitor. I-Palomid 529 (P529) inqanda i-TORC1 kunye ne-TORC2 i-complexes kwaye ibonisa zombini ukuthintela ukubonakaliswa kwe-Akt kunye ne-mTOR ebonisa ngokufanayo kwi-tumor kunye ne-vasculature. Kwaboniswa ukuba i-P529 inqanda ukukhula kwe-tumor, i-angiogenesis, kunye nokuhamba kwe-vascular permeability. Igcine imiba eluncedo ye-tumor vascular normalization ethi irapamycin iqhayisa. Nangona kunjalo, i-P529 ibonise inzuzo eyongezelelweyo yokuvala umqondiso we-pAktS473 ohambelana nokuvala i-TORC2 kuzo zonke iiseli kwaye ngaloo ndlela idlula iilophu zempendulo ezikhokelela ekwandiseni umqondiso we-Akt kwezinye iiseli zethumba. (Umthombo: Cancer Res 008;68(22):9551?–7). |
| CPD100634 | BGT226-maleate | I-BGT226 yi-phosphatidylinositol 3-kinase (PI3K) inhibitor enokuthi ibe nomsebenzi we-antineoplastic. I-PI3K inhibitor BGT226 inhibits ngokukodwa i-PIK3 kwi-PI3K / AKT kinase (okanye iprotein kinase B) indlela yokubonisa, enokubangela ukuhanjiswa kwe-cytosolic Bax kwi-membrane yangaphandle ye-mitochondrial, ukwandisa ukugqithisa kwe-mitochondrial membrane; Ukufa kweeseli ze-aptotic kunokubangela. I-Bax lilungu le-proapoptotic Bcl2 intsapho yeeprotheni. |
| CPD100633 | WYE-125132 | I-WYE-125132, eyaziwa ngokuba yi-WYE-132, inamandla kakhulu, i-ATP-ekhuphisanayo, kunye ne-mTOR kinase inhibitor ethile (IC(50): 0.19 +/- 0.07 nmol/L;>5,000-fold selective against PI3Ks). I-WYE-132 inhibited mTORC1 kunye ne-mTORC2 kwiimodeli ezahlukeneyo zomhlaza kwi-vitro nakwi-vivo. Okubalulekileyo, ngokuhambelana nokukhutshwa kwemfuza ye-mTORC2, i-WYE-132 ejoliswe kwi-P-AKT (S473) kunye nomsebenzi we-AKT ngaphandle kokunciphisa kakhulu izinga lokuzinza kwe-PI3K / PDK1 ye-biomarker yomsebenzi we-P-AKT (T308), ukugqamisa umgaqo obalaseleyo kunye othe ngqo. ye-AKT nge-mTORC2 kwiiseli zomhlaza. |
| CPD100632 | Vistusertib | I-Vistusertib, ekwaziwa ngokuba yi-AZD2014, sisithinteli se-bioavailable ngomlomo se-mammalian target of rapamycin (mTOR) enomsebenzi we-antineoplastic. I-mTOR kinase inhibitor AZD2014 inqanda umsebenzi we-mTOR, onokubangela ukufakwa kwe-tumor cell apoptosis kunye nokuncipha kwe-tumor cell proliferation. I-mTOR, i-serine / threonine kinase elawulwa kwiindidi ezahlukeneyo ze-tumor, idlala indima ebalulekileyo ezantsi kwindlela yokubonisa i-PI3K / Akt / mTOR. |
| CPD100631 | WYE-354 | I-WYE-354 yi-inhibitor enamandla ye-cell-permeable inhibitor ye-mTOR (IC50 = 4.3 nM) evimba ukubonakaliswa nge-mTOR complex 1 (mTORC1) kunye ne-mTORC2. |
| CPD100630 | Gedatolisib | I-Gedatolisib, eyaziwa ngokuba yi-PKI-587 kunye ne-PF-05212384, i-arhente ejolise kwi-phosphatidylinositol 3 kinase (PI3K) kunye nethagethi ye-mammalian ye-rapamycin (mTOR) kwi-PI3K / mTOR indlela yokubonisa, kunye nomsebenzi onokuthi ube ne-antineoplastic. Emva kokulawulwa kwe-intravenous, i-PI3K/mTOR kinase inhibitor PKI-587 inhibits zombini i-PI3K kunye ne-mTOR kinases, enokuthi ibangele i-apoptosis kunye nokuvinjelwa kokukhula kweeseli zomhlaza ezigqithise i-PI3K / mTOR. Ukusebenza kwendlela ye-PI3K / mTOR ikhuthaza ukukhula kweeseli, ukusinda, kunye nokuchasana ne-chemotherapy kunye ne-radiotherapy; I-mTOR, i-serine/threonine kinase ezantsi kwe-PI3K, inokuthi isebenze ngokuzimeleyo kwi-PI3K. |
