| IKATI # | Igama Lomkhiqizo | Incazelo |
| I-CPD100904 | I-Voruciclib | I-Voruciclib, eyaziwa nangokuthi i-P1446A-05, iyi-protein kinase inhibitor eqondene ngqo ne-cyclin-dependent kinase 4 (CDK4) enekhono lomsebenzi we-antineoplastic. I-CDK4 inhibitor P1446A-05 ivimbela ngokuqondile ukuguqulwa kwesigaba se-CDK4-mediated G1-S, ukubopha ukujikeleza kwamaseli kanye nokuvimbela ukukhula kwamangqamuzana omdlavuza. I-serine/threonine kinase CDK4 itholakala kunkimbinkimbi enamabhayisikili ohlobo lwe-D-G1 futhi iyi-kinase yokuqala ukwenziwa isebenze phezu kokukhuthazwa kwe-mitogenic, ikhipha amaseli ukusuka esigabeni esithule ukuya esigabeni sokukhula samabhayisikili se-G1/S; Ama-CDK-cyclin complexes aboniswe njenge-phosphorylate the retinoblastoma (Rb) transcription factor ekuqaleni kwe-G1, asusa i-histone deacetylase (HDAC) futhi avimbe ukucindezelwa kokubhaliwe. |
| I-CPD100905 | I-Alvocidib | I-Alvocidib iyinhlanganisela ye-N-methylpiperidinyl chlorophenyl flavone yokwenziwa. Njenge-inhibitor ye-cyclin-dependent kinase, i-alvocidib inxusa ukuboshwa komjikelezo weseli ngokuvimbela i-phosphorylation ye-cyclin-dependent kinases (CDKs) kanye nenkulumo elawula phansi ye-cyclin D1 kanye ne-D3, okuholela ekuboshweni komjikelezo weseli ye-G1 kanye ne-apoptosis. Le ejenti iphinde ibe inhibitor yokuncintisana yomsebenzi we-adenosine triphosphate. Hlola izivivinyo zomtholampilo ezisebenzayo noma izivivinyo zomtholampilo ezivaliwe usebenzisa lesi sisebenzeli. |
| I-CPD100906 | BS-181 | I-BS-181 iyi-CDK inhibitor ekhetha kakhulu ye-CDK7 ene-IC(50) engu-21 nmol/L. Ukuhlolwa kwamanye ama-CDK kanye namanye ama-kinase angu-69 kubonise ukuthi i-BS-181 ivimbele i-CDK2 kuphela ekugxilweni okungaphansi kuka-1 micromol/L, i-CDK2 ivinjwe ngokuphindwe izikhathi ezingu-35 ngokunamandla (IC(50) 880 nmol/L) kune-CDK7. Kumaseli e-MCF-7, i-BS-181 ivimbele i-phosphorylation yama-CDK7 substrates, yakhuthaza ukuboshwa komjikelezo wamaseli kanye ne-apoptosis ukuvimbela ukukhula kwemigqa yamangqamuzana omdlavuza, futhi yabonisa imiphumela ye-antitumor ku-vivo. |
| I-CPD100907 | I-Rivicclib | I-Riviciclib, eyaziwa nangokuthi i-P276-00, iyi-flavone ne-cyclin encike kinase (CDK) inhibitor enomsebenzi ongaba khona we-antineoplastic. I-P276-00 ibopha ngokukhetha futhi ivimbele i-Cdk4/cyclin D1, i-Cdk1/cyclin B ne-Cdk9/cyclin T1, i-serine/threonine kinases edlala izindima ezibalulekile ekulawuleni umjikelezo weseli nokwanda kwamaselula. Ukuvinjelwa kwalawa ma-kinase kuholela ekuboshweni komjikelezo weseli ngesikhathi soguquko lwe-G1/S, ngaleyo ndlela kuholele ekungenweni kwe-apoptosis, kanye nokuvinjwa kokwanda kwamaseli wesimila. |
| I-CPD100908 | I-MC180295 | I-MC180295 iyi-CDK9 inhibitor ekhetha kakhulu (IC50 = 5 nM). (I-MC180295 inomsebenzi obanzi wokulwa nomdlavuza ku-vitro futhi iyasebenza kumamodeli womdlavuza we-vivo. Ukwengeza, i-CDK9 inhibition izwela i-immune checkpoint inhibitor α-PD-1 ku-vivo, ikwenze kube okuhlosiwe okuhle kakhulu kwe-epigenetic therapy yomdlavuza. |
| 1073485-20-7 | LDC000067 | I-LDC000067 iyi-CDK9 inhibitor enamandla futhi ekhethayo. I-LDC000067 ivinjwe ukulotshwa kwe-in vitro ngendlela yokuncintisana ne-ATP futhi encike kumthamo. Ukuchazwa kwephrofayili ye-Gene yamaseli aphathwe nge-LDC000067 kubonise ukuncishiswa okukhethiwe kwama-mRNA ahlala isikhathi esifushane, okuhlanganisa nabalawuli ababalulekile bokwanda kanye ne-apoptosis. Ukuhlaziywa kwe-de novo RNA synthesis kuphakamise indima enhle ehlukahlukene ye-CDK9. Ezingeni lamangqamuzana namaselula, i-LDC000067 iphinde yakhiqiza imiphumela yesici sokuvinjwa kwe-CDK9 njengokumisa isikhashana okuthuthukisiwe kwe-RNA polymerase II ezakhini zofuzo futhi, okubaluleke kakhulu, ukufakwa kwe-apoptosis kumaseli omdlavuza. I-LDC000067 ivimbela ukuloba kwe-in vitro okuncike ku-P-TEFb. Idala i-apoptosis ku-vitro kanye ne-vivo ihlanganiswe ne-BI 894999. |
| I-CPD100910 | I-SEL120-34A | I-SEL120-34A iyi-CDK8 inhibitor enamandla futhi ekhethayo esebenza kumaseli e-AML anamazinga aphezulu e-serine phosphorylation ye-STAT1 kanye ne-STAT5 transactivation domain. I-EL120-34A ivimbela i-phosphorylation ye-STAT1 S727 ne-STAT5 S726 kumaseli omdlavuza ku-vitro. Ngokuqhubekayo, ukulawulwa kwe-STATs- kanye nokuloba okuncike ku-NUP98-HOXA9- kuye kwaqashelwa njengendlela ehamba phambili yokusebenza ku-vivo. |
| Idatha ye-CPDB1540 | MSC2530818 | I-MSC2530818 iyi-CDK8 Inhibitor Enamandla, Ekhethayo, kanye ne-Olly Bioavailable Bioavailable ene-CDK8 IC50 = 2.6 nM; Ukubikezela kwe-PK yomuntu: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F > 75%. |
| Idatha ye-CPDB1574 | I-CYC-065 | I-CYC065 iyisizukulwane sesibili, etholakala ngomlomo i-ATP-competitive inhibitor ye-CDK2/CDK9 kinases enekhono le-antineoplastic kanye nemisebenzi ye-chemoprotective. |
| Idatha ye-CPDB1594 | THZ531 | I-THZ531 iyi-covalent CDK12 kanye ne-CDK13 covalent inhibitor. I-Cyclin-dependent kinases 12 kanye ne-13 (CDK12 ne-CDK13) idlala indima ebalulekile ekulawuleni ukulotshwa kofuzo. |
| Idatha ye-CPDB1587 | THZ2 | I-THZ2, i-analog ye-THZ1, enamandla okwelapha umdlavuza webele we-Triple-negative (TNBC), iyi-CDK7 inhibitor enamandla futhi ekhethayo enqoba ukungazinzi kwe-THZ1 ku-vivo. I-IC50: CDK7= 13.9 nM; Amaseli e-TNBC= 10 nM |
