| MPAKA # | Dzina lazogulitsa | Kufotokozera |
| CPD100904 | Voruciclib | Voruciclib, yomwe imadziwikanso kuti P1446A-05, ndi protein kinase inhibitor yeniyeni ya cyclin-dependent kinase 4 (CDK4) yokhala ndi ntchito yoletsa antiineoplastic. CDK4 inhibitor P1446A-05 makamaka imaletsa kusintha kwa gawo la CDK4-mediated G1-S, kumanga ma cell njinga ndikuletsa kukula kwa maselo a khansa. Serine / threonine kinase CDK4 imapezeka mu zovuta ndi D-mtundu wa G1 cyclins ndipo ndiye kinase woyamba kutsegulidwa pa mitogenic stimulation, kutulutsa maselo kuchokera pa siteji ya quiescent kupita ku G1 / S kukula kwa njinga; Ma CDK-cyclin complexes awonetsedwa kuti ali ndi phosphorylate the retinoblastoma (Rb) transcript factor kumayambiriro kwa G1, kuchotsa histone deacetylase (HDAC) ndikuletsa kuponderezedwa kwa transcriptional. |
| CPD100905 | Alvocidib | Alvocidib ndi mankhwala opangidwa ndi N-methylpiperidinyl chlorophenyl flavone. Monga inhibitor ya cyclin-dependent kinase, alvocidib imapangitsa kuti maselo asamamangidwe poletsa phosphorylation ya cyclin-dependent kinases (CDKs) ndi kutsika-regulating cyclin D1 ndi D3 mawu, zomwe zimapangitsa kuti G1 cell cycle kumangidwa ndi apoptosis. Wothandizira uyu ndiyenso mpikisano woletsa ntchito ya adenosine triphosphate. Yang'anani mayesero azachipatala omwe akugwira ntchito kapena mayesero otsekedwa achipatala pogwiritsa ntchito wothandizira uyu. |
| CPD100906 | Chithunzi cha BS-181 | BS-181 ndi choletsa kwambiri cha CDK cha CDK7 chokhala ndi IC(50) ya 21 nmol/L. Kuyesedwa kwa ma CDK ena komanso ma kinase ena 69 kunawonetsa kuti BS-181 idangoletsa CDK2 pamalo otsika kuposa 1 micromol/L, pomwe CDK2 idaletsedwa 35-fold less potently (IC(50) 880 nmol/L) kuposa CDK7. M'maselo a MCF-7, BS-181 inaletsa phosphorylation ya magawo a CDK7, kulimbikitsa kumangidwa kwa ma cell cycle ndi apoptosis kuti alepheretse kukula kwa maselo a khansa, ndikuwonetsa zotsatira za antitumor mu vivo. |
| CPD100907 | Rivicclib | Riviciclib, yemwe amadziwikanso kuti P276-00, ndi flavone ndi cyclin dependent kinase (CDK) inhibitor yomwe ingathe kuchitapo kanthu. P276-00 imamangiriza ndikuletsa Cdk4 / cyclin D1, Cdk1 / cyclin B ndi Cdk9 / cyclin T1, serine / threonine kinases yomwe imagwira ntchito yofunika kwambiri pakuwongolera ma cell ndi kuchuluka kwa ma cell. Kuletsa kwa kinasewa kumabweretsa kumangidwa kwa ma cell panthawi ya kusintha kwa G1/S, zomwe zimapangitsa kuti apoptosis alowe, ndikuletsa kuchulukana kwa maselo otupa. |
| CPD100908 | Mtengo wa MC180295 | MC180295 ndi yosankha kwambiri CDK9 inhibitor (IC50 = 5 nM). (MC180295 ili ndi ntchito zambiri zotsutsana ndi khansa mu vitro ndipo imagwira ntchito mu zitsanzo za khansa ya vivo. Kuwonjezera apo, CDK9 inhibition imalimbikitsa chitetezo cha mthupi α-PD-1 mu vivo, ndikupangitsa kuti ikhale chandamale chabwino kwambiri cha epigenetic therapy ya khansa. |
| 1073485-20-7 | LDC000067 | LDC000067 ndi choletsa champhamvu komanso chosankha cha CDK9. LDC000067 inhibited in vitro transcript mu ATP-mpikisano komanso kutengera mlingo. Kufotokozera kwa ma gene kuma cell omwe amathandizidwa ndi LDC000067 kunawonetsa kuchepetsedwa kosankha kwa ma mRNA osakhalitsa, kuphatikiza owongolera ofunikira pakuchulukira ndi apoptosis. Kuwunika kwa kaphatikizidwe ka de novo RNA kunawonetsa mbali zambiri zabwino za CDK9. Pama cell ndi ma cell, LDC000067 idatulutsanso zotsatira za CDK9 zoletsa monga kuyimitsidwa kwa RNA polymerase II pamajini ndipo, chofunikira kwambiri, kulowetsedwa kwa apoptosis m'maselo a khansa. LDC000067 imalepheretsa kulembedwa kwa P-TEFb mu vitro. Imapangitsa apoptosis mu vitro ndi mu vivo kuphatikiza BI 894999. |
| CPD100910 | Chithunzi cha SEL120-34A | SEL120-34A ndi CDK8 inhibitor yamphamvu komanso yosankha yogwira ntchito m'maselo a AML okhala ndi serine phosphorylation ya STAT1 ndi STAT5 transactivation domains. EL120-34A imalepheretsa phosphorylation ya STAT1 S727 ndi STAT5 S726 m'maselo a khansa mu vitro. Nthawi zonse, kuwongolera kwa STATs- ndi NUP98-HOXA9- kutengera zolembera kwawonedwa ngati njira yayikulu yochitira zinthu mu vivo. |
| Chithunzi cha CPDB1540 | MSC2530818 | MSC2530818 ndi Mphamvu Yamphamvu, Yosankha, ndi Olly Bioavailable CDK8 Inhibitor yokhala ndi CDK8 IC50 = 2.6 nM; Ulosi wa PK waumunthu: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F> 75%. |
| Mtengo wa CPDB1574 | Mtengo wa CYC-065 | CYC065 ndi yachiwiri, yopezeka pakamwa ya ATP-competitive inhibitor ya CDK2/CDK9 kinases yomwe ingathe kuchitapo kanthu poletsa anti-antineoplastic ndi chemoprotective. |
| Mtengo wa CPDB1594 | Mtengo wa THZ531 | THZ531 ndi covalent CDK12 ndi CDK13 covalent inhibitor. Cyclin-dependent kinases 12 ndi 13 (CDK12 ndi CDK13) amatenga gawo lofunikira pakuwongolera kalembedwe ka jini. |
| Mtengo wa CPDB1587 | THZ2 | THZ2, analogi ya THZ1, yokhoza kuchiza khansa ya m'mawere ya Triple-negative (TNBC), ndi CDK7 inhibitor yamphamvu komanso yosankha yomwe imagonjetsa kusakhazikika kwa THZ1 mu vivo. IC50: CDK7= 13.9 nM; Maselo a TNBC = 10 nM |
