| CAT # | Inoa Huahana | wehewehe |
| CPD100654 | PD-169316 | ʻO PD-169316 kahi mea hoʻokae koho o p38 MAPK. Kāohi ia i ka p38 MAPK me kahi IC50 o 89 nM. PD169316, pale i ka hoʻololi ʻana i ka mea ulu beta-i hoʻokomo ʻia i ka hōʻailona Smad i loko o nā maʻi maʻi ovarian kanaka. |
| CPD100653 | LDN-193189 | ʻO LDN193189 kahi mea hoʻopaneʻe BMP liʻiliʻi liʻiliʻi me IC50 o 5 a me 30 nM no ALK2 a me ALK3. ʻO LDN193189 hoʻi e kāohi i ka BMP type I receptors ALK6 (TGFβ1 / BMP hōʻailona) a me ka phosphorylation SMAD ma hope. |
| CPD100652 | K02288 | ʻO K02288 kahi mea paʻa ikaika o ka hōʻailona BMP. Loaʻa iā K02288 ka hana in vitro e kūʻē iā ALK2 ma nā haʻahaʻa nanomolar haʻahaʻa e like me ka hui alakaʻi o kēia manawa LDN-193189. K02288 i keakea pono i ka BMP-induced Smad alahele me ka hoʻopili ʻole ʻana i ka hōʻailona TGF-β a me ka dorsalization o nā embryos zebrafish. |
| CPD100650 | SB-431542 | ʻO SB-431542 kahi mea hoʻopaneʻe mole liʻiliʻi liʻiliʻi o ke ʻano I TGF-beta receptor, ma kahi papa o nā laina cell glioma malignant kanaka. Ua kāohi ʻo SB-431542 i ka phosphorylation a me ka translocation nuklea o nā SMAD, nā mea hoʻolaha intracellular o ka hōʻailona TGF-beta, me ka hoʻemi ʻana o ka TGF-beta-mediated transcription. Eia kekahi, ua kāohi ʻo SB-431542 i ka hōʻike ʻana o ʻelua mau hopena koʻikoʻi o ka TGF-beta-vascular endothelial growth factor a me ka plasminogen activator inhibitor-1. |
| CPD100649 | GW788388 | ʻO GW788388 kahi mea hou TGF-beta type I receptor inhibitor me ka hoʻomaikaʻi maikaʻi ʻana o ka pharmacokinetic profile i hoʻohālikelike ʻia me SB431542. Ua aʻo mākou i kona hopena i loko o ka vitro a ʻike ʻia ua kāohi ia i nā hana TGF-beta type I a me ke ʻano II receptor kinase, akā ʻaʻole ia o ka iwi pili morphogenic protein type II receptor. Eia hou, ua ālai ia i ka TGF-beta-induced Smad activation and target gene expression, oiai e emi ana ka epithelial-mesenchymal transitions a me ka fibrogenesis. |
| CPD100648 | SB-525334 | ʻO SB525334 kahi mea hoʻopaneʻe ikaika a koho i ka mea hoʻololi hoʻololi ulu-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). Ua kāohi ʻo SB525334 i ka hana ALK5 kinase me kahi IC (50) o 14.3 nM a ua like ʻo ia me 4-fold ka liʻiliʻi o ka ikaika ma ke ʻano he inhibitor o ALK4 (IC(50) = 58.5 nM). ʻAʻole hana ʻo SB-525334 ma ke ʻano he mea paʻa o ALK2, ALK3, a me ALK6 (IC(50) > 10,000 nM). I loko o nā ho'āʻo pūnaewele, SB-525334 (1 microM) ālai i ka TGF-beta1-induced phosphorylation a me ka nuclear translocation o Smad2/3 i loko o ka renal proximal tubule cell a kāohi i ka TGF-beta1-induced piʻi i ka plasminogen activator inhibitor-1 (PAI-1). ) a me ka procollagen alpha1(I) mRNA hōʻike i loko o A498 renal epithelial carcinoma cell. |
| CPD100647 | BIBF0775 | ʻO BIBF0775 kahi mea pale o ka mea hoʻololi ulu β receptor I (TGFβRI). Ua hōʻike ʻia ka nānā ʻana o ka hoʻolālā X-ray ua komo ʻo BIBF0775 i loko o ka domain kinase o TGFβRI |
| CPD100646 | LY3023414 | ʻO LY3023414 kahi mole liʻiliʻi i hōʻike ʻia i loko o ka vitro he mea hoʻokūkū hoʻokūkū koho ATP o PI3Kα a me mTOR, DNA-PK, a me nā lālā ʻohana PI3K papa ʻē aʻe. In vitro, ua hōʻike ʻo LY3023414 i ka hana inhibitory e kūʻē i ka PI3K a me ka mTOR i loko o nā cell tumor, a me ka hana antiproliferative a me nā hopena pōʻai cell. Eia hou, in vitro, LY3023414 inhibits hiki o PI3K a me mTOR i phosphorylate substrates ma ke ala PI3K / mTOR. Ke noiʻi ʻia nei ʻo LY3023414 ma kahi hoʻāʻo hoʻokolohua maʻi. |
| CPD100645 | Onatasertib | ʻO CC-223 kahi mea hoʻopaneʻe waha i loaʻa i ka mea hoʻomake ʻia o ka rapamycin (mTOR) me ka hana antineoplastic. ʻO ka mTOR kinase inhibitor CC-223 ke kāohi i ka hana o ka mTOR, hiki ke hopena i ka hoʻokomo ʻana o ka apoptosis cell tumo a me ka emi ʻana o ka hoʻonui ʻana o nā cell tumor. ʻO ka mTOR, kahi kinase serine/threonine i hoʻoponopono ʻia i loko o nā ʻano ʻokoʻa like ʻole, he hana koʻikoʻi i lalo i ke ala hōʻailona PI3K/AKT/mTOR, i hoʻopaʻa pinepine ʻia i nā maʻi maʻi kanaka. |
| CPD100644 | ʻO Bimiralisib | ʻO Bimiralisib, ka mea i kapa ʻia ʻo PQR309, he mea hoʻopaneʻe pan o ka phosphoinositide-3-kinases (PI3K) a me ka mea hoʻopaneʻe o ka pahuhopu mammalian o rapamycin (mTOR), me ka hana antineoplastic. PI3K/mTOR kinase inhibitor PQR309 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, i ka liʻiliʻi loa, mTOR kinase, hiki ke hopena i ka apoptosis cell tumo a me ka ulu ʻana i loko o nā cell overexpressing PI3K/mTOR. ʻO ka hoʻoulu ʻana o ke ala PI3K/mTOR e hoʻoikaika i ka ulu ʻana o ke kelepona, ola, a me ke kū'ē ʻana i ka chemotherapy a me ka radiotherapy. |
| CPD100643 | CZ415 | ʻO CZ415 kahi mea hoʻopaʻapaʻa mTOR hoʻokūkū ikaika ATP me ka koho koho ʻole ʻia ma luna o nā kinase ʻē aʻe (IC50 = 14.5 nM IC50 no pS6RP a me 14.8 nM no pAKT) me ka permeability cell maikaʻi loa (Kd app = 6.9 nM). ʻO nā waiwai Pharmacokinetic o ka hoʻomaʻemaʻe haʻahaʻa a me ka bioavailability waha maikaʻi i hōʻike i ke kūpono o CZ415 no ka holomua i nā haʻawina in vivo. Hōʻike ʻo CZ415 i kahi mole kūpono no ka noiʻi lāʻau lapaʻau o ka hana pathophysiological mTOR i vivo. |
| CPD100642 | GDC-0084 | ʻO GDC-0084, ka mea i ʻike ʻia ʻo RG7666 a me Paxalisib, he phosphatidylinositol 3-kinase (PI3K) inhibitor me ka hana antineoplastic. PI3K inhibitor GDC-0084 kiko'ī 'ana i ka PI3K ma ka PI3K/AKT kinase (ai ole protein kinase B) ala ala hoailona, pela e keakea ai i ka ho'āla 'ana o ke ala hōʻailona PI3K. Hiki paha i kēia ke pale i ka ulu ʻana o ke kelepona a me ke ola ʻana i nā heluna cell tumor susceptible. Hoʻopili pinepine ʻia ka hoʻāla ʻana o ke ala hōʻailona PI3K me ka tumorigenesis. |
| CPD100641 | CC-115 | ʻO CC-115 he mea hoʻopaneʻe ʻelua o ka DNA-dependent protein kinase (DNA-PK) a me ka pahuhopu mammalian o rapamycin (mTOR), me ka hana antineoplastic hiki ke hana. Hoʻopaʻa ʻo CC-115 i ka hana a DNA-PK a me ka raptor-mTOR (TOR complex 1 a i ʻole TORC1) a me rictor-mTOR (TOR complex 2 a i ʻole TORC2), hiki ke alakaʻi i ka hōʻemi ʻana i ka hoʻonui ʻana o nā cell cancer cell e hōʻike ana. DNA-PK a me TOR. ʻO DNA-PK, he serine/threonine kinase a he lālā o ka PI3K-pili kinase subfamily o ka protein kinases, ua hoʻāla ʻia ma luna o ka pōʻino DNA a he hana koʻikoʻi i ka hoʻoponopono ʻana i nā haʻihaʻi DNA kaulua ma o ka DNA nonhomologous end joining (NHEJ) alahele. . |
| CPD100640 | XL388 | ʻO XL388 kahi Papa Hou o ka Highly Potent, Selective, ATP-Competitive, a me nā mea hōʻemi waha o ka Mammalian Target o Rapamycin (mTOR). Ua kāohi ʻo XL388 i ka phosphorylation cellular o ka mTOR complex 1 (p-p70S6K, pS6, a me p-4E-BP1) a me ka mTOR complex 2 (pAKT (S473)) substrates. Ua hōʻike ʻo XL388 i nā lāʻau lapaʻau maikaʻi a me ka hoʻolaha waha i nā ʻano he nui me ka bioavailability haʻahaʻa. ʻO ka hoʻoponopono waha o XL388 i nā ʻiole athymic nude i hoʻokomo ʻia me nā xenografts tumo kanaka i hāʻawi ʻia i ka hana antitumor koʻikoʻi a hilinaʻi. |
| CPD100639 | GDC-0349 | ʻO GDC-0349 kahi mole lāʻau anticaner liʻiliʻi, i hoʻomohala ʻia e Genentech. Ma Iulai 2012, ua waiho ʻo Genentech i ka hoʻāʻo pae I o GDC-0349 no ka loiloi ʻana i ka palekana a me ka hoʻomanawanui o GDC-0349 i nā maʻi me nā kiʻekiʻe kūloko a i ʻole Metastatic Solid Tumors a i ʻole Non Hodgkin's Lymphoma. |
| CPD100638 | ETP-46464 | ʻO ETP46464 ka mea hoʻopaneʻe o ka DNA damage response kinase Ataxia-telangiectasia mutated (ATM)- a me Rad3-related (ATR). |
| CPD100637 | ALA-600 | ʻO WAY-600 kahi mea hoʻokūkū ikaika, ATP-hoʻokūkū a koho i ka mTOR me IC50 o 9 nM. |
| CPD100636 | WYE-687 | ʻO WYE-687 kahi mea hoʻokūkū ikaika a ATP-hoʻokūkū a koho i ka mTOR me IC50 o 7 nM. |
| CPD100635 | Palomid-529 | ʻO Palomid 529, i ʻike ʻia ʻo P529, he mea hoʻopaneʻe PI3K/Akt/mTOR. Palomid 529 (P529) kaohi i ka TORC1 a me TORC2 paʻakikī a hōʻike i ka pale ʻana i ka hōʻailona Akt a me ka hōʻailona mTOR e like me ka tumora a me ka vasculature. Ua hōʻike ʻia ua pale ʻo P529 i ka ulu ʻana o ka tumo, angiogenesis, a me ka permeability vascular. Ua mālama ʻo ia i nā ʻano pono o ka hoʻomaʻamaʻa ʻana i ka maʻi maʻi maʻi e kaena ʻo rapamycin. Eia nō naʻe, ua hōʻike ʻo P529 i ka pōmaikaʻi hou o ka pale ʻana i ka hōʻailona pAktS473 e kūlike me ka hoʻopaʻa ʻana iā TORC2 i nā cell āpau a no laila ke kaʻe ʻana i nā puka manaʻo e alakaʻi ai i ka hoʻonui ʻana i ka hōʻailona Akt i kekahi mau cell tumor. (Source: Cancer Res 008;68(22):9551?–7). |
| CPD100634 | BGT226-kāne | ʻO ka BGT226 he mea hoʻopaneʻe phosphatidylinositol 3-kinase (PI3K) me ka hana antineoplastic. ʻO ka PI3K inhibitor BGT226 keʻakeʻa pono i ka PIK3 ma ke ala hōʻailona PI3K / AKT kinase (aiʻole ka protein kinase B), hiki ke hoʻoulu i ka unuhiʻana o ka cytosolic Bax i ka membrane waho mitochondrial, e hoʻonui ana i ka mitochondrial membrane permeability; hiki mai paha ka make a apoptotic cell. He lālā ʻo Bax o ka ʻohana proapoptotic Bcl2 o nā protein. |
| CPD100633 | WYE-125132 | ʻO WYE-125132, i kapa ʻia ʻo WYE-132, he mea hoʻokūkū ikaika loa, ATP-competitive, a kikoʻī mTOR kinase inhibitor (IC(50): 0.19 +/- 0.07 nmol/L; >5,000-fold selective versus PI3Ks). Ua kāohi ʻo WYE-132 i ka mTORC1 a me ka mTORC2 i nā ʻano maʻi maʻi like ʻole i vitro a i vivo. ʻO ka mea nui, e kūlike me ka genetic ablation o mTORC2, WYE-132 i manaʻo ʻia ʻo P-AKT(S473) a me ka hana AKT me ka ʻole o ka hoʻohaʻahaʻa ʻana i ka pae paʻa o ka PI3K/PDK1 hana biomarker P-AKT(T308), e hōʻike ana i kahi hoʻoponopono koʻikoʻi a pololei. o AKT e ka mTORC2 i loko o nā pūnana maʻi maʻi. |
| CPD100632 | Vistusertib | ʻO Vistusertib, ka mea i ʻike ʻia ʻo AZD2014, he mea hoʻopaneʻe bioavailable o ka mammalian target o rapamycin (mTOR) me ka hana antineoplastic. ʻO ka mTOR kinase inhibitor AZD2014 ke kāohi i ka hana o ka mTOR, hiki ke hopena i ka hoʻokomo ʻana i ka apoptosis cell tumo a me ka emi ʻana o ka hoʻonui ʻana o nā cell tumor. ʻO ka mTOR, kahi kinase serine/threonine i hoʻoponopono ʻia i loko o nā ʻano maʻi ʻokoʻa, he hana koʻikoʻi i lalo i ke ala hōʻailona PI3K/Akt/mTOR. |
| CPD100631 | WYE-354 | ʻO WYE-354 kahi mea hoʻopaneʻe maʻemaʻe cell-permeable o mTOR (IC50 = 4.3 nM) e poloka ana i ka hōʻailona ma o ka mTOR complex 1 (mTORC1) a me ka mTORC2. |
| CPD100630 | Gedatolisib | ʻO Gedatolisib, ka mea i kapa ʻia ʻo PKI-587 a me PF-05212384, he ʻelele e kuhikuhi ana i ka phosphatidylinositol 3 kinase (PI3K) a me ka pahuhopu mammalian o rapamycin (mTOR) ma ke ala hōʻailona PI3K/mTOR, me ka hana antineoplastic hiki ke hana. Ma ka hoʻokele intravenous, PI3K/mTOR kinase inhibitor PKI-587 ke kāohi i ka PI3K a me ka mTOR kinases, hiki ke hopena i ka apoptosis a me ka ulu ʻana o ka maʻi kanesa e hōʻike ana i ka PI3K/mTOR. ʻO ka hoʻoulu ʻana o ke ala PI3K/mTOR e hoʻoikaika i ka ulu ʻana o ke kelepona, ola, a me ke kū'ē ʻana i ka chemotherapy a me ka radiotherapy; mTOR, he serine/threonine kinase ma lalo o PI3K, hiki ke ho'ā 'ia me ke kū'oko'a o PI3K. |
