| CAT # | Khoom npe | Kev piav qhia |
| PIB 100654 | PIB-169316 | PD-169316 yog ib qho kev xaiv inhibitor ntawm p38 MAPK. Nws inhibits p38 MAPK nrog IC50 ntawm 89 nM. PD169316, inhibits kev loj hlob ntawm beta-induced Smad signaling nyob rau hauv tib neeg lub zes qe menyuam qog noj ntshav. |
| PIB 100653 | TIAB SA-193189 | LDN193189 yog ib qho muaj zog me me molecule BMP inhibitor nrog IC50 ntawm 5 thiab 30 nM rau ALK2 thiab ALK3, feem. LDN193189 kuj inhibits BMP hom I receptors ALK6 (TGFβ1 / BMP signaling) thiab tom qab SMAD phosphorylation. |
| PIB 100652 | k02288 ua | K02288 yog ib qho muaj zog inhibitor ntawm BMP signaling. K02288 muaj kev ua haujlwm hauv vitro tiv thaiv ALK2 ntawm qhov tsawg nanomolar concentrations zoo ib yam li cov hlau lead tam sim no LDN-193189. K02288 tshwj xeeb inhibited txoj kev BMP-induced Smad yam tsis muaj kev cuam tshuam rau TGF-β signaling thiab induced dorsalization ntawm zebrafish embryos |
| PIB 100650 | SIB-431542 | SB-431542 yog ib qho tshiab me me molecule inhibitor ntawm hom I TGF-beta receptor, ntawm lub vaj huam sib luag ntawm tib neeg malignant glioma cell kab. SB-431542 thaiv cov phosphorylation thiab nuclear translocation ntawm SMADs, intracellular mediators ntawm TGF-beta signaling, nrog txo TGF-beta-mediated transcription. Tsis tas li ntawd, SB-431542 inhibited qhov kev qhia ntawm ob qhov tseem ceeb ntawm TGF-beta-vascular endothelial kev loj hlob yam thiab plasminogen activator inhibitor-1. |
| PAB 100649 | wb 788388 | GW788388 yog tus tshiab TGF-beta hom I receptor inhibitor nrog kev txhim kho pharmacokinetic profile piv nrog SB431542. Peb tau kawm nws cov nyhuv hauv vitro thiab pom tias nws inhibited ob qho tib si TGF-beta hom I thiab hom II receptor kinase kev ua ub no, tab sis tsis yog ntawm cov pob txha morphogenic protein ntau hom II receptor. Tsis tas li ntawd, nws tau thaiv TGF-beta-induced Smad activation thiab lub hom phiaj gene qhia, thaum txo qis epithelial-mesenchymal hloov thiab fibrogenesis. |
| PIB 100648 | SIB-525334 | SB525334 yog ib qho muaj zog thiab xaiv inhibitor ntawm kev hloov pauv kev loj hlob-beta1 (TGF-beta1) receptor, activin receptor-zoo li kinase (ALK5). SB525334 inhibited ALK5 kinase kev ua haujlwm nrog IC (50) ntawm 14.3 nM thiab yog kwv yees li 4-fold tsawg zog raws li inhibitor ntawm ALK4 (IC(50) = 58.5 nM). SB-525334 yog inactive raws li ib tug inhibitor ntawm ALK2, ALK3, thiab ALK6 (IC(50) > 10,000 nM). Hauv kev soj ntsuam ntawm tes, SB-525334 (1 microM) thaiv TGF-beta1-induced phosphorylation thiab nuclear translocation ntawm Smad2/3 nyob rau hauv lub raum proximal tubule hlwb thiab inhibited TGF-beta1-induced nce nyob rau hauv plasminogen activator inhibitor-1 (PAI-1). ) thiab procollagen alpha1(I) mRNA qhia hauv A498 lub raum epithelial carcinoma cells. |
| PAB 100647 | PAB 0775 | BIBF0775 yog ib qho inhibitor ntawm kev hloov pauv kev loj hlob β receptor I (TGFβRI). X-ray qauv tsom xam pom tias BIBF0775 tsau rau hauv kinase domain ntawm TGFβRI |
| PIB 100646 | TIAB SA 3023414 | LY3023414 yog ib qho me me molecule uas tau pom nyob rau hauv vitro los ua ib qho kev xaiv ATP-kev sib tw inhibitor ntawm PI3Kα thiab mTOR, DNA-PK, thiab lwm chav kawm I PI3K tsev neeg. Hauv vitro, LY3023414 tau qhia txog kev ua haujlwm inhibitory tiv thaiv PI3K thiab mTOR hauv cov qog hlwb, nrog rau kev ua haujlwm tiv thaiv kab mob thiab cov teebmeem ntawm lub voj voog ntawm tes. Tsis tas li ntawd, hauv vitro, LY3023414 inhibits lub peev xwm ntawm PI3K thiab mTOR rau phosphorylate substrates hauv PI3K / mTOR txoj hauv kev. LY3023414 tab tom raug tshawb xyuas nyob rau theem kuv kuaj mob. |
| PIB 100645 | Onatasertib | CC-223 yog ib qho tshuaj uas muaj nyob rau hauv qhov ncauj inhibitor ntawm lub hom phiaj mammalian ntawm rapamycin (mTOR) uas muaj peev xwm ua haujlwm antineoplastic. mTOR kinase inhibitor CC-223 inhibits qhov kev ua ntawm mTOR, uas yuav ua rau induction ntawm qog cell apoptosis thiab txo cov qog cell proliferation. mTOR, ib qho serine / threonine kinase uas tau kho nyob rau hauv ntau hom qog, ua lub luag haujlwm tseem ceeb hauv PI3K / AKT / mTOR txoj kev taw qhia, uas feem ntau ua rau tib neeg mob qog noj ntshav. |
| PIB 100644 | Bimiralisib | Bimiralisib, tseem hu ua PQR309, yog ib qho kev hais lus bioavailable pan inhibitor ntawm phosphoinositide-3-kinases (PI3K) thiab inhibitor ntawm cov hom phiaj tsiaj ntawm rapamycin (mTOR), muaj peev xwm ua haujlwm antineoplastic. PI3K / mTOR kinase inhibitor PQR309 inhibits PI3K kinase isoforms alpha, beta, gamma thiab delta thiab, rau qhov tsawg dua, mTOR kinase, uas yuav ua rau qog cell apoptosis thiab kev loj hlob inhibition hauv hlwb overexpressing PI3K / mTOR. Kev ua kom txoj hauv kev PI3K / mTOR txhawb nqa kev loj hlob ntawm tes, muaj sia nyob, thiab tiv thaiv ob qho tib si kev kho mob thiab xov tooj cua. |
| PIB 100643 | CZ415 | CZ415 yog lub zog ATP-kev sib tw mTOR inhibitor nrog kev xaiv tsis tau pom dua dhau los ntawm lwm cov kinase (IC50 = 14.5 nM IC50 rau pS6RP thiab 14.8 nM rau pAKT) nrog rau cov cell permeability zoo heev (Kd app = 6.9 nM). Pharmacokinetic cov khoom ntawm kev tshem tawm nruab nrab thiab qhov ncauj zoo bioavailability pom qhov tsim nyog ntawm CZ415 rau kev nce mus rau hauv vivo kev tshawb fawb. CZ415 sawv cev rau qhov zoo tshaj plaws molecule rau kev tshawb nrhiav tshuaj ntawm mTOR pathophysiological lub luag haujlwm hauv vivo. |
| PIB 100642 | TSI-0084 | GDC-0084, tseem hu ua RG7666 thiab Paxalisib, yog ib qho phosphatidylinositol 3-kinase (PI3K) inhibitor uas muaj peev xwm ua haujlwm antineoplastic. PI3K inhibitor GDC-0084 tshwj xeeb inhibits PI3K hauv PI3K / AKT kinase (los yog protein kinase B) taw qhia txoj hauv kev, yog li inhibiting kev ua kom ntawm PI3K signaling pathway. Qhov no yuav ua rau inhibition ntawm kev loj hlob ntawm tes thiab ciaj sia nyob rau hauv cov neeg mob qog nqaij hlav. Kev ua kom lub PI3K signaling txoj kev yog feem ntau txuam nrog cov qog nqaij hlav. |
| PIB 100641 | TSI-115 | CC-115 yog ib qho inhibitor dual ntawm DNA-dependent protein kinase (DNA-PK) thiab mammalian lub hom phiaj ntawm rapamycin (mTOR), uas muaj peev xwm ua haujlwm antineoplastic. CC-115 khi rau thiab inhibits cov kev ua ntawm DNA-PK thiab ob qho tib si raptor-mTOR (TOR complex 1 los yog TORC1) thiab rictor-mTOR (TOR complex 2 los yog TORC2), uas tej zaum yuav ua rau txo qis ntawm cellular proliferation ntawm cov qog nqaij hlav cancer qhia. DNA-PK thiab TOR. DNA-PK, ib tug serine/threonine kinase thiab ib tug tswv cuab ntawm PI3K-hais txog kinase subfamily ntawm protein kinases, yog qhib rau DNA puas thiab plays lub luag hauj lwm tseem ceeb hauv kev kho ob-stranded DNA so ntawm DNA nonhomologous kawg koom (NHEJ) txoj kev. . |
| PIB 100640 | XLIV 388 | XL388 yog ib chav kawm tshiab uas muaj peev xwm, xaiv tau, ATP-Competitive, thiab Orally Bioavailable Inhibitors ntawm Mammalian Target ntawm Rapamycin (mTOR). XL388 inhibited cellular phosphorylation ntawm mTOR complex 1 (p-p70S6K, pS6, thiab p-4E-BP1) thiab mTOR complex 2 (pAKT (S473)) substrates. XL388 tso tawm cov tshuaj pharmacokinetics zoo thiab qhov ncauj raug nyob rau hauv ntau hom nrog nruab nrab bioavailability. Kev tswj hwm qhov ncauj ntawm XL388 rau cov nas athymic liab qab implanted nrog tib neeg qog xenografts tau txais txiaj ntsig tseem ceeb thiab koob tshuaj tiv thaiv kab mob. |
| PAB 100639 | TSI-0349 | GDC-0349 yog ib tug me me molecule anticaner tshuaj neeg sib tw, yog tsim los ntawm Genentech. Raws li lub Xya hli ntuj 2012, Genentech tau ua tiav theem kuv sim ntawm GDC-0349 rau kev soj ntsuam Kev Nyab Xeeb thiab Kev Tiv Thaiv ntawm GDC-0349 hauv Cov Neeg Mob Nrog Hauv Zos Advanced lossis Metastatic Solid Tumors lossis Non Hodgkin's Lymphoma. |
| PAB 100638 | ETP-46464 | ETP46464 yog ib qho inhibitor ntawm DNA kev puas tsuaj teb kinase Ataxia-telangiectasia mutated (ATM)- thiab Rad3-txog (ATR). |
| PAB 100637 | KEV-600 | WAY-600 yog lub zog, ATP-kev sib tw thiab xaiv inhibitor ntawm mTOR nrog IC50 ntawm 9 nM |
| PIB 100636 | TSW-687 | WYE-687 yog lub zog thiab ATP-kev sib tw thiab xaiv inhibitor ntawm mTOR nrog IC50 ntawm 7 nM. |
| PIB 100635 | Palomid-529 | Palomid 529, tseem hu ua P529, yog ib qho tshiab PI3K / Akt / mTOR inhibitor. Palomid 529 (P529) inhibits TORC1 thiab TORC2 complexes thiab qhia ob qho tib si inhibition ntawm Akt signaling thiab mTOR signaling zoo sib xws hauv qog thiab vasculature. Nws tau pom tias P529 inhibited qog loj hlob, angiogenesis, thiab vascular permeability. Nws khaws cov txiaj ntsig zoo ntawm cov qog vascular normalization uas rapamycin khav theeb. Txawm li cas los xij, P529 tau qhia txog qhov txiaj ntsig ntxiv ntawm kev thaiv pAktS473 kev taw qhia zoo ib yam nrog kev thaiv TORC2 hauv txhua lub hlwb thiab yog li hla cov lus tawm tswv yim uas ua rau muaj kev nce Akt signaling hauv qee cov qog hlwb. (Source: Cancer Res 008; 68(22): 9551?–7). |
| PIB 100634 | BGT226-maleate | BGT226 yog ib qho phosphatidylinositol 3-kinase (PI3K) inhibitor uas muaj peev xwm ua haujlwm antineoplastic. PI3K inhibitor BGT226 tshwj xeeb inhibits PIK3 hauv PI3K / AKT kinase (los yog protein kinase B) kev taw qhia, uas tuaj yeem ua rau kev hloov pauv ntawm cytosolic Bax mus rau mitochondrial txheej membrane, nce mitochondrial membrane permeability; apoptotic cell tuag yuav tshwm sim. Bax yog ib tug tswv cuab ntawm proapoptotic Bcl2 tsev neeg ntawm cov proteins. |
| PIB 100633 | WYE-125132 | WYE-125132, tseem hu ua WYE-132, yog lub zog muaj zog, ATP-kev sib tw, thiab tshwj xeeb mTOR kinase inhibitor (IC(50): 0.19 +/- 0.07 nmol / L; > 5,000-fold xaiv piv rau PI3Ks). WYE-132 inhibited mTORC1 thiab mTORC2 hauv ntau hom mob qog noj ntshav hauv vitro thiab hauv vivo. Qhov tseem ceeb, ua raws li cov caj ces ablation ntawm mTORC2, WYE-132 lub hom phiaj P-AKT (S473) thiab AKT muaj nuj nqi yam tsis muaj kev txo qis hauv lub xeev ntawm PI3K / PDK1 kev ua ub no biomarker P-AKT (T308), qhia txog qhov tseem ceeb thiab ncaj qha kev cai. ntawm AKT los ntawm mTORC2 hauv cov qog nqaij hlav cancer. |
| PIB 100632 | Vistusertib | Vistusertib, tseem hu ua AZD2014, yog ib qho kev hais lus bioavailable inhibitor ntawm lub hom phiaj mammalian ntawm rapamycin (mTOR) uas muaj peev xwm ua haujlwm antineoplastic. mTOR kinase inhibitor AZD2014 inhibits qhov kev ua ntawm mTOR, uas yuav ua rau induction ntawm qog cell apoptosis thiab txo cov qog cell proliferation. mTOR, ib qho serine / threonine kinase uas tau hloov kho nyob rau hauv ntau hom qog, ua lub luag haujlwm tseem ceeb hauv PI3K / Akt / mTOR txoj kev taw qhia. |
| PIB 100631 | TSW-354 | WYE-354 yog ib qho muaj zog ntawm tes-permeable inhibitor ntawm mTOR (IC50 = 4.3 nM) uas thaiv kev taw qhia los ntawm ob qho tib si mTOR complex 1 (mTORC1) thiab mTORC2. |
| PIB 100630 | Gedatolisib | Gedatolisib, tseem hu ua PKI-587 thiab PF-05212384, yog tus neeg sawv cev tsom rau phosphatidylinositol 3 kinase (PI3K) thiab mammalian lub hom phiaj ntawm rapamycin (mTOR) hauv PI3K / mTOR kev taw qhia txoj hauv kev, nrog rau cov kev ua haujlwm antineoplastic. Raws li kev tswj hwm txoj hlab ntshav, PI3K / mTOR kinase inhibitor PKI-587 inhibits PI3K thiab mTOR kinases, uas tuaj yeem ua rau apoptosis thiab kev loj hlob inhibition ntawm cov qog nqaij hlav cancer overexpressing PI3K / mTOR. Kev ua kom txoj hauv kev PI3K / mTOR txhawb kev loj hlob ntawm tes, muaj sia nyob, thiab tiv thaiv kev siv tshuaj khomob thiab xov tooj cua; mTOR, ib qho serine / threonine kinase downstream ntawm PI3K, kuj tseem tuaj yeem ua haujlwm ywj pheej ntawm PI3K. |
