| CAT # | Igama lemveliso | Inkcazo |
| CPD100904 | I-Voruciclib | I-Voruciclib, ekwabizwa ngokuba yi-P1446A-05, yiprotein kinase inhibitor ethe ngqo kwi-cyclin-dependent kinase 4 (CDK4) enomsebenzi we-antineoplastic. I-CDK4 inhibitor P1446A-05 inqanda ngokukodwa inguqu yesigaba se-CDK4-mediated G1-S, ukubamba i-cell cycling kunye nokuthintela ukukhula kweeseli zomhlaza. I-serine / threonine kinase CDK4 ifumaneka kwi-complex kunye ne-D-type G1 cyclins kwaye yi-kinase yokuqala ukuba isebenze ngokuvuselela i-mitogenic, ukukhulula iiseli ukusuka kwinqanaba elipholileyo ukuya kwinqanaba lokukhula kwebhayisikili ye-G1 / S; I-CDK-cyclin complexes iboniswe ukuba i-phosphorylate i-retinoblastoma (Rb) i-transcription factor in early G1, displaceing histone deacetylase (HDAC) kunye nokuthintela ukunyanzeliswa kwe-transcriptional. |
| CPD100905 | Alvocidib | I-Alvocidib yi-synthetic N-methylpiperidinyl chlorophenyl flavone compound. Njenge-inhibitor ye-cyclin-dependent kinase, i-alvocidib yenza ukuba kubanjwe umjikelezo weseli ngokuthintela i-phosphorylation ye-cyclin-dependent kinases (CDKs) kunye ne-down-regulating cyclin D1 kunye ne-D3 expression, okubangelwa ukubanjwa kwe-cell cycle ye-G1 kunye ne-apoptosis. Le arhente ikwayi-inhibitor ekhuphisanayo yomsebenzi we-adenosine triphosphate. Khangela izilingo zeklinikhi ezisebenzayo okanye izilingo zekliniki ezivaliweyo usebenzisa le arhente. |
| CPD100906 | BS-181 | I-BS-181 yi-CDK inhibitor ekhethiweyo kakhulu ye-CDK7 ene-IC (50) ye-21 nmol / L. Uvavanyo lwezinye ii-CDKs kunye nenye i-69 kinases ibonise ukuba i-BS-181 ivimbele i-CDK2 kuphela kwiindawo ezingaphantsi kwe-1 micromol / L, kunye ne-CDK2 ivinjelwe i-35-fold less potently (IC (50) 880 nmol / L) kune-CDK7. Kwiiseli ze-MCF-7, i-BS-181 inqande i-phosphorylation ye-CDK7 substrates, ikhuthaze ukubanjwa komjikelo weseli kunye ne-apoptosis ukuthintela ukukhula kwemigca yeseli yomhlaza, kwaye ibonise iziphumo ze-antitumor kwi-vivo. |
| CPD100907 | Rivicclib | I-Riviciclib, eyaziwa nangokuthi i-P276-00, i-flavone kunye ne-cyclin exhomekeke kwi-kinase (CDK) inhibitor enokuthi isebenze i-antineoplastic. I-P276-00 ibophelela ngokukhethekileyo kwaye inqanda i-Cdk4 / i-cyclin D1, i-Cdk1 / i-cyclin B kunye ne-Cdk9 / i-cyclin T1, i-serine / i-threonine kinases edlala indima ebalulekileyo ekulawuleni umjikelezo weseli kunye nokunyuka kwamaselula. Ukuvinjelwa kwezi kinases kukhokelela ekubanjweni komjikelo weeseli ngexesha lenguqu ye-G1/S, ngaloo ndlela ikhokelela ekungenweni kwe-apoptosis, kunye nokuthintela ukwanda kweeseli zethumba. |
| CPD100908 | MC180295 | I-MC180295 yi-CDK9 inhibitor ekhethiweyo kakhulu (IC50 = 5 nM). (I-MC180295 inomsebenzi obanzi wokuchasana nomhlaza kwi-vitro kwaye iyasebenza kwiimodeli zomhlaza we-vivo. Ukongeza, i-CDK9 inhibition ivakalisa i-immune checkpoint inhibitor α-PD-1 kwi-vivo, iyenza ibe yinjongo egqwesileyo yonyango lwe-epigenetic lomhlaza. |
| 1073485-20-7 | LDC000067 | I-LDC000067 yi-CDK9 inhibitor enamandla kwaye ekhethiweyo. I-LDC000067 inhibited in vitro transcription ngendlela ye-ATP-ekhuphisanayo kunye ne-dose-dependent. Ukuchazwa kweprofayili ye-Gene yeeseli eziphathwe nge-LDC000067 kubonise ukucuthwa okukhethiweyo kwee-mRNA ezihlala ixesha elifutshane, kubandakanywa nabalawuli ababalulekileyo bokwanda kunye ne-apoptosis. Uhlalutyo lwe-de novo RNA synthesis lucebise indima ebanzi eyahlukahlukeneyo ye-CDK9. Kwinqanaba lemolekyuli kunye neselula, i-LDC000067 iphinde yavelisa iziphumo ze-CDK9 inhibition ezifana nokuphuculwa kokunqumamisa kwe-RNA polymerase II kwiigenes kwaye, okona kubaluleke kakhulu, ukufakwa kwe-apoptosis kwiiseli zomhlaza. I-LDC000067 inqanda i-P-TEFb exhomekeke kwi-vitro transcription. Yenza i-apoptosis kwi-vitro kunye ne-vivo ngokudibanisa ne-BI 894999. |
| CPD100910 | SEL120-34A | I-SEL120-34A yi-CDK8 inhibitor enamandla kwaye ekhethiweyo esebenzayo kwiiseli ze-AML ezinamazinga aphezulu e-serine phosphorylation ye-STAT1 kunye ne-STAT5 ye-transactivation domains. I-EL120-34A inqanda i-phosphorylation ye-STAT1 S727 kunye ne-STAT5 S726 kwiiseli zomhlaza kwi-vitro. Ngokuqhubekayo, ukulawulwa kwe-STATs- kunye ne-NUP98-HOXA9- exhomekeke kwi-transcript ibonwe njengendlela ebalaseleyo yesenzo kwi-vivo. |
| CPDB1540 | MSC2530818 | I-MSC2530818 yi-CDK8 Inhibitor enamandla, eKhethekileyo, kunye ne-Olly Bioavailable Bioavailable CDK8 IC50 = 2.6 nM; Ukuqikelelwa kwe-PK yomntu: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F > 75%. |
| CPDB1574 | I-CYC-065 | I-CYC065 isizukulwana sesibini, i-ATP-competitive inhibitor efumaneka ngomlomo ye-CDK2 / CDK9 kinases enezinto ezinokubakho ze-antineoplastic kunye ne-chemoprotective. |
| CPDB1594 | THZ531 | I-THZ531 yi-CDK12 ehlangeneyo kunye ne-CDK13 covalent inhibitor. I-Cyclin-dependent kinases 12 kunye ne-13 (CDK12 kunye ne-CDK13) idlala indima ebalulekileyo ekulawuleni ukubhaliswa kofuzo. |
| CPDB1587 | THZ2 | I-THZ2, i-analog ye-THZ1, enokukwazi ukunyanga umhlaza webele we-Triple-negative (TNBC), i-CDK7 inhibitor enamandla kwaye ekhethiweyo eyoyisa ukungazinzi kwe-THZ1 kwi-vivo. IC50: CDK7= 13.9 nM; Iiseli zeTNBC= 10 nM |
