| KATSE # | Lebitso la Sehlahiswa | Tlhaloso |
| CPD100904 | Voruciclib | Voruciclib, eo hape e tsejoang e le P1446A-05, ke protheine kinase inhibitor e khethehileng bakeng sa cyclin-dependent kinase 4 (CDK4) e nang le ts'ebetso e ka bang teng ea antineoplastic. CDK4 inhibitor P1446A-05 ka ho khetheha e thibela phetoho ea mohato oa CDK4-mediated G1-S, ho tšoara libaesekele tsa sele le ho thibela kholo ea lisele tsa mofetše. CDK4 ea serine / threonine kinase e fumanoa ka mokhoa o rarahaneng o nang le li-cyclins tsa mofuta oa D-mofuta oa G1 'me ke kinase ea pele e sebelisoang holim'a ts'usumetso ea mitogenic, e lokolla lisele ho tloha sethaleng se khutsitseng ho ea sethaleng sa G1 / S sa baesekele ea kholo; Li-CDK-cyclin complexes li bontšitsoe ho phosphorylate the retinoblastoma (Rb) transcription factor qalong ea G1, ho tlosa histone deacetylase (HDAC) le ho thibela khatiso ea transcriptional. |
| CPD100905 | Alvocidib | Alvocidib ke motsoako oa maiketsetso oa N-methylpiperidinyl chlorophenyl flavone. Joalo ka inhibitor ea cyclin-dependent kinase, alvocidib e etsa hore ho ts'oaroe ha cell cycle ka ho thibela phosphorylation ea cyclin-dependent kinases (CDKs) le ka ho theola taolo ea cyclin D1 le polelo ea D3, e fellang ka ho ts'oaroa ha lisele tsa G1 le apoptosis. Moemeli ona hape ke inhibitor ea tlholisano ea ts'ebetso ea adenosine triphosphate. Sheba liteko tse sebetsang tsa tleliniki kapa liteko tse koetsoeng tsa bongaka u sebelisa moemeli enoa. |
| CPD100906 | BS-181 | BS-181 ke CDK inhibitor e khethang haholo bakeng sa CDK7 e nang le IC(50) ea 21 nmol/L. Liteko tsa li-CDK tse ling hammoho le li-kinase tse ling tse 69 li bonts'itse hore BS-181 e thibela CDK2 feela maemong a tlase ho 1 micromol/L, 'me CDK2 e thibetsoe ka makhetlo a 35 ka matla (IC(50) 880 nmol/L) ho feta CDK7. Liseleng tsa MCF-7, BS-181 e thibetse phosphorylation ea li-substrates tsa CDK7, e khothalelitse ho ts'oaroa ha potoloho ea lisele le apoptosis ho thibela kholo ea lisele tsa mofetše, mme e bonts'a litlamorao tsa antitumor ho vivo. |
| CPD100907 | Rivicclib | Riviciclib, e tsejoang hape e le P276-00, ke inhibitor ea flavone le cyclin dependent kinase (CDK) e nang le ts'ebetso e ka bang teng ea antineoplastic. P276-00 e khetha ho tlama le ho thibela Cdk4 / cyclin D1, Cdk1 / cyclin B le Cdk9 / cyclin T1, serine / threonine kinases e phethang karolo ea bohlokoa taolong ea potoloho ea lisele le ho ata ha lisele. Ho thibela li-kinase tsena ho lebisa ho ts'oaroe ha potoloho ea lisele nakong ea phetoho ea G1 / S, ka hona ho lebisa ho induction ea apoptosis, le ho thibela ho ata ha lisele tsa tumor. |
| CPD100908 | MC180295 | MC180295 ke CDK9 inhibitor e khethang haholo (IC50 = 5 nM). (MC180295 e na le ts'ebetso e pharaletseng ea anti-cancer in vitro mme e sebetsa hantle mefuteng ea mofets'e oa vivo. Ho feta moo, CDK9 inhibition e hlokomelisa ho immune checkpoint inhibitor α-PD-1 in vivo, e etsa hore e be sepheo se setle sa kalafo ea epigenetic ea mofets'e. |
| 1073485-20-7 | LDC000067 | LDC000067 ke inhibitor e matla le e khethang ea CDK9. LDC000067 e thibetsoe ho ngoloa ka har'a vitro ka mokhoa oa tlholisano oa ATP le o itšetlehileng ka tekanyo. Tlhaloso ea liphatsa tsa lefutso ea lisele tse tšoaroang ka LDC000067 e bonts'itse phokotso e ikhethileng ea li-mRNA tsa nakoana, ho kenyelletsa le balaoli ba bohlokoa ba ho ata le apoptosis. Tlhahlobo ea de novo RNA synthesis e khothalelitse karolo e fapaneng e ntle ea CDK9. Boemong ba limolek'hule le liselefouno, LDC000067 e hlahisitse litlamorao tsa thibelo ea CDK9 joalo ka khefutso e ntlafalitsoeng ea RNA polymerase II liphatseng tsa lefutso, 'me haholo-holo, ho kenngoa ha apoptosis liseleng tsa mofetše. LDC000067 e thibela ho ngoloa ha P-TEFb e itšetlehileng ka in vitro. E kenya apoptosis in vitro le in vivo hammoho le BI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A ke CDK8 inhibitor e matla le e khethang e sebetsang liseleng tsa AML tse nang le maemo a phahameng a serine phosphorylation ea STAT1 le STAT5 transactivation domains. EL120-34A e thibela phosphorylation ea STAT1 S727 le STAT5 S726 liseleng tsa mofetše ka vitro. Ka mokhoa o ts'oanang, taolo ea STATs- le NUP98-HOXA9- e itšetlehileng ka transcript e 'nile ea hlokomeloa e le mokhoa o ka sehloohong oa ts'ebetso ka vivo. |
| CPDB1540 | MSC2530818 | MSC2530818 ke CDK8 Inhibitor e Matla, e Khethollang, le ea Molomo e nang le CDK8 IC50 = 2.6 nM; Polelo ea PK ea Motho: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F > 75%. |
| CPDB1574 | CYC-065 | CYC065 ke ea moloko oa bobeli, e fumanehang ka molomo ATP-competitive inhibitor ea CDK2/CDK9 kinases e nang le mesebetsi e ka bang teng ea antineoplastic le chemoprotective. |
| CPDB1594 | THZ531 | THZ531 ke covalent CDK12 le CDK13 covalent inhibitor. Cyclin-dependent kinases 12 le 13 (CDK12 le CDK13) li bapala karolo ea bohlokoa taolong ea mongolo oa liphatsa tsa lefutso. |
| CPDB1587 | THZ2 | THZ2, analoge ea THZ1, e nang le monyetla oa ho phekola mofetše oa matsoele oa Triple-negative (TNBC), ke CDK7 inhibitor e matla le e khethang e hlolang ho se tsitse ha THZ1 ka vivo. IC50: CDK7 = 13.9 nM; Lisele tsa TNBC= 10 nM |
