| CAT # | Product Name | Tsanangudzo |
| CPD100904 | Voruciclib | Voruciclib, inozivikanwawo seP1446A-05, iprotein kinase inhibitor yakanangana necyclin-dependent kinase 4 (CDK4) ine inogona kuita antineoplastic chiitiko. CDK4 inhibitor P1446A-05 inonyanya kurambidza CDK4-mediated G1-S chikamu shanduko, kusunga sero bhasikoro uye inhibiting cancer cell kukura. Iyo serine/threonine kinase CDK4 inowanikwa mune yakaoma ine D-mhando G1 cyclins uye ndiyo yekutanga kinase kuti ishandiswe pane mitogenic kukurudzira, kuburitsa masero kubva padanho rakanyarara kupinda muG1/S kukura bhasikoro nhanho; CDK-cyclin complexes yakaratidzwa kune phosphorylate iyo retinoblastoma (Rb) chinyorwa chekunyora mukutanga kweG1, ichibvisa histone deacetylase (HDAC) uye ichivharira kudzvinyirirwa kwezvinyorwa. |
| CPD100905 | Alvocidib | Alvocidib is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. Se inhibitor ye cyclin-inotsamira kinase, alvocidib induces cell cycle kusungwa nekudzivirira phosphorylation ye cyclin-dependent kinases (CDKs) uye nekudzika-inotonga cyclin D1 uye D3 kutaura, zvichiita kuti G1 cell cycle kusungwa uye apoptosis. Uyu mumiririri zvakare inokwikwidza inhibitor yeadenosine triphosphate basa. Tarisa uone kushanda kwekiriniki miedzo kana kuvharwa kwekiriniki miedzo uchishandisa mumiririri uyu. |
| CPD100906 | BS-181 | BS-181 inonyatso kusarudza CDK inhibitor yeCDK7 ine IC(50) ye21 nmol/L. Kuongororwa kwemamwe maCDK pamwe nemamwe makumi matanhatu nemapfumbamwe kinase kwakaratidza kuti BS-181 yakangovharira CDK2 pamitsetse yakaderera pane 1 micromol/L, neCDK2 ichivharirwa makumi matatu neshanu zvishoma zvine simba (IC(50) 880 nmol/L) pane CDK7. Mumasero eMCF-7, BS-181 yakadzivisa phosphorylation yeCDK7 substrates, yakasimudzira kusungwa kwesero cycle uye apoptosis kudzivisa kukura kwekenza cell mitsara, uye yakaratidza antitumor madhara mu vivo. |
| CPD100907 | Rivicclib | Riviciclib, inozivikanwawo seP276-00, ndeye flavone uye cyclin inotsamira kinase (CDK) inhibitor ine inogona kuita antineoplastic chiitiko. P276-00 inosarudza inosunga uye inhibits Cdk4 / cyclin D1, Cdk1 / cyclin B uye Cdk9 / cyclin T1, serine / threonine kinases inobata mabasa anokosha mukugadzirisa kwesero uye kuwedzera kwemasero. Kudzivirirwa kweaya kinase kunotungamira kusungwa kwesero kusungwa panguva yeG1/S shanduko, zvichizotungamira mukuiswa kweapoptosis, uye kuvharirwa kwebundu cell kuwanda. |
| CPD100908 | MC180295 | MC180295 inonyanya kusarudza CDK9 inhibitor (IC50 = 5 nM). (MC180295 ine yakakura anti-cancer chiitiko mu vitro uye inoshanda mu vivo cancer modhi. Uyezve, CDK9 inhibition inosimudzira kune immune checkpoint inhibitor α-PD-1 mu vivo, zvichiita kuti ive chinangwa chakanakisa che epigenetic kurapa kenza. |
| 1073485-20-7 | LDC000067 | LDC000067 ine simba uye inosarudza CDK9 inhibitor. LDC000067 inhibited in vitro transcription nenzira yeATP-yemakwikwi uye inotsamira muyero. Gene expression profiling yemasero akabatwa neLDC000067 yakaratidza kuderedzwa kwakasarudzika kwemamRNAs enguva pfupi, kusanganisira akakosha ekudzora kupararira uye apoptosis. Ongororo ye de novo RNA synthesis yakakurudzira basa rakasiyana-siyana rakanaka reCDK9. Payero yemamorekuru nemaserura, LDC000067 yakadzokorodza maitiro eCDK9 inhibition senge kukwidziridzwa kumbomira kweRNA polymerase II pamajini uye, zvakanyanya kukosha, kuiswa kweapoptosis mumasero egomarara. LDC000067 inhibits P-TEFb-inotsamira mu vitro transcription. Inoita kuti apoptosis in vitro uye mu vivo musanganiswa neBI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A ine simba uye inosarudza CDK8 inhibitor inoshanda muAML maseru ane yakakwira serine phosphorylation yeSTAT1 uye STAT5 transactivation domains. EL120-34A inhibits phosphorylation yeSTAT1 S727 uye STAT5 S726 mumasero ekenza mu vitro. Sezvineiwo, kudzorwa kweSTATs- uye NUP98-HOXA9- inotsamira kunyorwa yakaonekwa seyakanyanya nzira yekuita mu vivo. |
| CPDB1540 | MSC2530818 | MSC2530818 ine Simba, Inosarudza, uye Nemuromo Bioavailable CDK8 Inhibitor ine CDK8 IC50 = 2.6 nM; Kufanotaura kwevanhu PK: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F > 75%. |
| CPDB1574 | CYC-065 | CYC065 chizvarwa chechipiri, chinowanikwa nemuromo ATP-competitive inhibitor yeCDK2/CDK9 kinases ine zvingangoita antineoplastic uye chemoprotective zviitiko. |
| CPDB1594 | THZ531 | THZ531 ndeye covalent CDK12 uye CDK13 covalent inhibitor. Cyclin-inotsamira kinases 12 uye 13 (CDK12 uye CDK13) inotamba mabasa akakosha mukutonga kwekunyorwa kwemajini. |
| CPDB1587 | THZ2 | THZ2, analogi yeTHZ1, ine mukana wekurapa Triple-negative cancer cancer (TNBC), ine simba uye inosarudza CDK7 inhibitor inokunda kusagadzikana kweTHZ1 in vivo. IC50: CDK7= 13.9 nM; TNBC maseru= 10 nM |
