| PUSI # | Igoa Oloa | Fa'amatalaga |
| CPD100904 | Voruciclib | Voruciclib, lea e lauiloa foi o le P1446A-05, o se polotini kinase inhibitor faapitoa mo le cyclin-faalagolago kinase 4 (CDK4) ma gaioiga antineoplastic gafatia. O le CDK4 inhibitor P1446A-05 fa'apitoa e fa'alavelaveina le CDK4-mediated G1-S vaega suiga, pu'eina le uila uila ma fa'alavelaveina le tuputupu a'e o le kanesa. O le serine / threonine kinase CDK4 o loʻo maua i totonu o se faʻalavelave faʻatasi ma D-ituaiga G1 cyclins ma o le kinase muamua lea e faʻagaoioia ile mitogenic stimulation, tuʻuina atu sela mai se tulaga quiescent i le G1 / S tuputupu aʻe uila laasaga; CDK-cyclin complexes ua faʻaalia e phosphorylate le retinoblastoma (Rb) transcription factor i le amataga o le G1, faʻateʻaina le histone deacetylase (HDAC) ma poloka le faʻasaʻoina o tusitusiga. |
| CPD100905 | Alvocidib | Alvocidib o le N-methylpiperidinyl chlorophenyl flavone fa'afefiloi. I le avea ai o se inhibitor o le cyclin-dependent kinase, alvocidib faʻaosofia le puʻeina o le taamilosaga e ala i le puipuia o le phosphorylation o cyclin-dependent kinases (CDKs) ma e ala i le faʻatonutonuina o le cyclin D1 ma le D3 faʻamatalaga, e mafua ai le G1 cell cycle puʻeina ma apoptosis. O lenei sooupu o se faʻatauvaʻa faʻatauvaʻa o gaioiga adenosine triphosphate. Siaki mo faʻataʻitaʻiga faʻapitoa faʻataʻitaʻiga poʻo faʻataʻitaʻiga tapuni faʻataʻitaʻiga e faʻaaoga ai lenei sooupu. |
| CPD100906 | BS-181 | O le BS-181 ose CDK e sili ona filifilia mo le CDK7 ma le IC(50) o le 21 nmol/L. O suʻesuʻega o isi CDKs faʻapea foʻi ma isi 69 kinases na faʻaalia ai naʻo le BS-181 na te taofia le CDK2 i faʻamaʻi maualalo ifo i le 1 micromol / L, ma le CDK2 o loʻo taofia 35-faʻaitiitia le malosi (IC (50) 880 nmol / L) nai lo CDK7. I sela MCF-7, BS-181 taofia le phosphorylation o le CDK7 substrates, siitia le taamilosaga o le puʻeina ma apoptosis e taofia ai le tuputupu aʻe o laina sela o le kanesa, ma faʻaalia aʻafiaga antitumor i vivo. |
| CPD100907 | Riviciclib | Riviciclib, lea e lauiloa foi o le P276-00, o se flavone ma cyclin dependent kinase (CDK) inhibitor ma gaioiga antineoplastic gafatia. P276-00 filifili faʻatasi ma faʻalavelave Cdk4 / cyclin D1, Cdk1 / cyclin B ma Cdk9 / cyclin T1, serine / threonine kinases o loʻo taʻalo i matafaioi taua i le faatonutonuina o le taamilosaga o le cell ma le faʻalauteleina o le telefoni. O le faʻasaina o nei kinases e taʻitaʻia ai le puʻeina o le taamilosaga i le taimi o le suiga o le G1 / S, ma oʻo atu ai i le faʻaogaina o le apoptosis, ma le faʻalavelaveina o le faʻateleina o le tumo. |
| CPD100908 | MC180295 | MC180295 o se inhibitor CDK9 sili ona filifilia (IC50 = 5 nM). (MC180295 o loʻo i ai le lautele o le gaioiga o le kanesa i vitro ma e aoga i faʻataʻitaʻiga o le kanesa in vivo. E le gata i lea, o le CDK9 inhibition e faʻaalia ai le puipuia o le puipuiga o le α-PD-1 i vivo, ma avea ai ma taulaʻiga sili mo togafitiga epigenetic o le kanesa. |
| 1073485-20-7 | LDC000067 | LDC000067 ose malosi ma filifili CDK9 inhibitor. LDC000067 faʻasaina in vitro transcription i se ATP-faʻatauva ma faʻalagolago i fua. O faʻamatalaga faʻamatalaga faʻamatalaga o sela na togafitia i le LDC000067 na faʻaalia ai se faʻaitiitiga filifilia o mRNA pupuu, e aofia ai faʻatonuga taua o le faʻateleina ma apoptosis. O le su'esu'ega o le de novo RNA synthesis na fa'ailoa mai ai se tulaga lelei tele o le CDK9. I le molecular ma le cellular level, LDC000067 toe gaosia aafiaga uiga o le CDK9 inhibition e pei o le faʻaleleia o le taofi o le RNA polymerase II i genes ma, sili ona taua, faʻaosoina o apoptosis i sela o le kanesa. LDC000067 faʻalavelave P-TEFb-faʻalagolago i le faʻaliliuga in vitro. Fa'aoso apoptosis in vitro ma in vivo fa'atasi ma BI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A o le malosi ma le filifilia CDK8 inhibitor o loʻo galue i sela AML ma maualuga maualuga o serine phosphorylation o STAT1 ma STAT5 transactivation domains. O le EL120-34A e taofia ai le phosphorylation o STAT1 S727 ma STAT5 S726 i sela o le kanesa in vitro. E le gata i lea, o tulafono faatonutonu o STATs- ma le NUP98-HOXA9-faʻalagolago transcription ua matauina o se faiga faʻapitoa o gaioiga i vivo. |
| CPDB1540 | MSC2530818 | MSC2530818 o se malosi, Filifilia, ma tautala tautala CDK8 Inhibitor ma CDK8 IC50 = 2.6 nM; Va'aiga PK tagata: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F > 75%. |
| CPDB1574 | CYC-065 | CYC065 o le lona lua-tupulaga, fa'atauva'a avanoa ATP inhibitors CDK2/CDK9 kinases ma mafai antineoplastic ma chemoprotective gaoioiga. |
| CPDB1594 | THZ531 | THZ531 o le CDK12 ma le CDK13 covalent inhibitor. Cyclin-faalagolago kinases 12 ma 13 (CDK12 ma CDK13) e taua tele i le faʻatonutonuina o faʻasologa o kenera. |
| CPDB1587 | THZ2 | THZ2, o se analog o le THZ1, faatasi ai ma le gafatia e togafitia ai le kanesa o le susu Tolu-negative (TNBC), o se inhibitor CDK7 malosi ma filifili lea e manumalo ai i le le mautonu o le THZ1 i vivo. IC50: CDK7= 13.9 nM; TNBC sela= 10 nM |
