| CAT # | Ingoa Hua | Whakaahuatanga |
| CPD100904 | Voruciclib | Ko Voruciclib, e mohiotia ana ko P1446A-05, he aukati kinase pūmua mo te kinase 4 (CDK4) e whakawhirinaki ana ki te cyclin me te mahi antineoplastic pea. Ko te aukati CDK4 P1446A-05 ka aukati i te whakawhitinga o te wahanga G1-S e CDK4-takawaenga, te hopu i te eke pahikara me te aukati i te tipu o te mate pukupuku. Ko te serine/threonine kinase CDK4 ka kitea i roto i te matatini me nga momo D-momo paihikara G1, a ko te kinase tuatahi ki te whakahohe i runga i te whakaihiihi mitogenic, te tuku i nga pūtau mai i te ata noho ki roto i te wahanga paihikara tipu G1/S; Kua whakaatuhia nga matatini CDK-cyclin ki te phosphorylate te retinoblastoma (Rb) tauwehe whakamaoritanga i te timatanga o te G1, te whakakore i te histone deacetylase (HDAC) me te aukati i te aukati tuhinga. |
| CPD100905 | Alvocidib | Ko Alvocidib he pūhui N-methylpiperidinyl chlorophenyl flavone. Hei aukati i te kinase cyclin-dependent, ka whakaawehia e alvocidib te hopu huringa pūtau ma te aukati i te phosphorylation o nga kinases cyclin-dependent (CDKs) me te whakaheke i te cyclin D1 me te D3, ka hua te hopukina huringa pūtau G1 me te apoptosis. Ko tenei kaihoko he kaiwhakataetae whakataetae mo te mahi adenosine triphosphate. Tirohia mo nga whakamatautau haumanu kaha, nga whakamatautau haumanu kati ranei ma te whakamahi i tenei kaihoko. |
| CPD100906 | BS-181 | Ko te BS-181 he aukati CDK tino whiriwhiri mo te CDK7 me te IC(50) o 21 nmol/L. Ko te whakamatautau i etahi atu CDK tae atu ki etahi atu 69 kinases i whakaatu ko te BS-181 anake te whakakore i te CDK2 i nga kohinga iti iho i te 1 micromol/L, me te CDK2 e aukati ana i te 35-fold iti ake te kaha (IC(50) 880 nmol/L) i te CDK7. I roto i nga pūtau MCF-7, ka aukati te BS-181 i te phosphorylation o nga taputapu CDK7, i whakatairanga i te hopu huringa pūtau me te apoptosis ki te aukati i te tipu o nga raina pūtau mate pukupuku, me te whakaatu i nga paanga antitumor i roto i te vivo. |
| CPD100907 | Riviciclib | Ko Riviciclib, e mohiotia ana ko P276-00, he flavone me te cyclin dependent kinase (CDK) aukati me te mahi antineoplastic pea. Ko te P276-00 ka herea, ka aukati i te Cdk4/cyclin D1, Cdk1/cyclin B me Cdk9/cyclin T1, serine/threonine kinases e whai waahi nui ana ki te whakahaere i te huringa o te pūtau me te whakatipu pūtau. Ko te whakakore i enei kinases ka arahi ki te hopu i te huringa pūtau i te wa o te whakawhitinga G1 / S, na reira ka arahina ki te whakauru o te apoptosis, me te aukati i te tipu o te pukupuku pukupuku. |
| CPD100908 | MC180295 | Ko te MC180295 he kaitautoko CDK9 tino whiriwhiri (IC50 = 5 nM). (MC180295 he mahi aukati-mate pukupuku i roto i te vitro me te whai hua i roto i nga tauira mate pukupuku in vivo. Hei taapiri, ko te aukati CDK9 e whakamohio ana ki te aukati α-PD-1 i roto i te vivo, ka waiho hei kaupapa pai mo te rongoa epigenetic o te mate pukupuku. |
| 1073485-20-7 | LDC000067 | Ko te LDC000067 he aukati CDK9 kaha me te whiriwhiri. Ko te LDC000067 i aukati i roto i te tuhi in vitro i roto i te ATP-whakataetae me te horopeta-whakawhirinaki. Ko te whakaaturanga whakaaturanga ira o nga pūtau i rongoahia ki te LDC000067 i whakaatu i te whakahekenga o nga mRNA poto poto, tae atu ki nga kaiwhakahaere nui o te tipu me te apoptosis. Ko te tātaritanga o te de novo RNA synthesis i kii i te whānuitanga pai o te CDK9. I te taumata ngota me te taumata pūtau, ka whakaputahia e LDC000067 nga ahuatanga o te aukati CDK9 penei i te whakaroa ake o te RNA polymerase II i runga i nga ira, me te mea nui, te whakaurunga o te apoptosis i roto i nga pūtau mate pukupuku. Ko te LDC000067 te aukati i te P-TEFb-whakawhirinaki i roto i te tuhinga in vitro. Ka whakakorikori i te apoptosis in vitro me in vivo me te BI 894999. |
| CPD100910 | SEL120-34A | Ko te SEL120-34A he kaiwawao CDK8 kaha me te whiriwhiri i roto i nga kamera AML me nga taumata teitei o te phosphorylation serine o nga rohe whakawhiti STAT1 me STAT5. Ko te EL120-34A ka whakakore i te phosphorylation o STAT1 S727 me STAT5 S726 i roto i nga pukupuku pukupuku i roto i te vitro. I nga wa katoa, kua kitea nga whakaritenga o nga tuhinga e whakawhirinaki ana ki te STATs- me te NUP98-HOXA9-he tikanga nui o te mahi i roto i te vivo. |
| CPDB1540 | MSC2530818 | Ko te MSC2530818 he Kaipupuri CDK8 Putea, Whiriwhiria, me te Oraly Bioavailable CDK8 me te CDK8 IC50 = 2.6 nM; Matapae PK tangata: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F > 75%. |
| CPDB1574 | CYC-065 | Ko te CYC065 he reanga tuarua, he aukati whakataetae ATP-whakataetae o nga kinases CDK2/CDK9 me nga mahi antineoplastic me te chemoprotective pea. |
| CPDB1594 | THZ531 | Ko te THZ531 ko te CDK12 me te CDK13 te aukati kovalent. Ko nga kinase 12 me te 13 (CDK12 me te CDK13) e whakawhirinaki ana ki te Cyclin e whai waahi nui ana i roto i te whakaritenga o te tuhi ira. |
| CPDB1587 | THZ2 | Ko te THZ2, he tairitenga o THZ1, me te kaha ki te rongoa i te mate pukupuku o te u Toru-kino (TNBC), he aukati CDK7 kaha me te kowhiria e hinga ai te koretake o te THZ1 in vivo. IC50: CDK7= 13.9 nM; Ngā pūtau TNBC= 10 nM |
