| nwamba # | Aha ngwaahịa | Nkọwa |
| CPD100904 | Voruciclib | Voruciclib, makwaara dị ka P1446A-05, bụ protein kinase inhibitor kpọmkwem maka cyclin-based kinase 4 (CDK4) nwere ọrụ antineoplastic. CDK4 inhibitor P1446A-05 na-egbochi mgbanwe oge nke CDK4-mediated G1-S, na-ejide ịnya igwe na igbochi uto mkpụrụ ndụ kansa. A na-achọta serine / threonine kinase CDK4 na mgbagwoju anya na ụdị D-ụdị G1 cyclins na ọ bụ kinase mbụ na-arụ ọrụ n'elu mkpali mitogenic, na-ahapụ mkpụrụ ndụ site na ọkwa nke quiescent n'ime G1 / S ịgba ígwè ịgba ígwè; E gosiputara ogige CDK-cyclin ka ọ na-eme ka phosphorylate ihe ntụgharị ederede retinoblastoma (Rb) n'oge G1, na-ewepụ histone deacetylase (HDAC) na igbochi mmegide transcriptional. |
| CPD100905 | Alvocidib | Alvocidib bụ ngwakọta N-methylpiperidinyl chlorophenyl flavone sịntetik. Dị ka onye na-egbochi cyclin-based kinase, alvocidib na-eme ka njide sel cell site na igbochi phosphorylation nke cyclin-dependent kinases (CDKs) na site na-achịkwa cyclin D1 na D3 okwu, na-akpata G1 cell cycle arrest na apoptosis. Onye nnọchi anya a bụkwa onye na-egbochi ọrụ adenosine triphosphate. Lelee maka nnwale ụlọ ọgwụ na-arụsi ọrụ ike ma ọ bụ nnwale ụlọ ọgwụ mechiri emechi site na iji nnọchite a. |
| CPD100906 | BS-181 | BS-181 bụ onye na-egbochi CDK nke ukwuu maka CDK7 nwere IC(50) nke 21 nmol/L. Nnwale nke CDK ndị ọzọ yana kinase 69 ọzọ gosiri na BS-181 na-egbochi CDK2 na mkpokọta dị ala karịa 1 micromol/L, na CDK2 na-egbochi 35-fold obere ike (IC(50) 880 nmol/L) karịa CDK7. N'ime mkpụrụ ndụ MCF-7, BS-181 gbochiri phosphorylation nke CDK7 substrates, na-akwalite njide okirikiri cell na apoptosis iji gbochie uto nke ahịrị mkpụrụ ndụ kansa, ma gosipụta mmetụta antitumor na vivo. |
| CPD100907 | Riviciclib | Riviciclib, nke a makwaara dị ka P276-00, bụ flavone na cyclin dabere kinase (CDK) inhibitor nwere ike antineoplastic ọrụ. P276-00 na-ahọrọ ma na-egbochi Cdk4/cyclin D1, Cdk1/cyclin B na Cdk9/cyclin T1, serine/threonine kinases nke na-arụ ọrụ dị mkpa na nhazi nke usoro cell na mgbasawanye cellular. Mgbochi nke kinases ndị a na-eduga na njide okirikiri cell n'oge mgbanwe G1/S, si otú ahụ na-eduga na ntinye nke apoptosis, na mgbochi nke mmụba cell tumor. |
| CPD100908 | MC180295 | MC180295 bụ onye na-egbochi CDK9 nke ukwuu (IC50 = 5 nM). (MC180295 nwere ọrụ mgbochi ọrịa cancer sara mbara na vitro ma dị irè na ụdị ọrịa cancer vivo. Ọzọkwa, mgbochi CDK9 na-eme ka ihe mgbochi mgbochi mgbochi α-PD-1 na vivo, na-eme ka ọ bụrụ ebumnuche magburu onwe ya maka ọgwụgwọ epigenetic nke ọrịa cancer. |
| 1073485-20-7 | LDC000067 | LDC000067 bụ ihe mgbochi CDK9 nwere ike na nhọrọ. LDC000067 amachibidoro ndegharị in vitro n'ụdị asọmpi ATP na dabere dose. Nkọwapụta mkpụrụ ndụ mkpụrụ ndụ nke e ji LDC000067 emeso ya gosipụtara mbelata nhọrọ nke mRNA dị mkpụmkpụ, gụnyere ndị na-achịkwa mkpa nke mgbasa na apoptosis. Nyocha nke njikọ de novo RNA na-atụ aro ọrụ dị oke mma nke CDK9. N'ọkwa molekụla na cellular, LDC000067 weputara mmetụta njirimara nke mgbochi CDK9 dị ka nkwụsịtụ RNA polymerase II na mkpụrụ ndụ ihe nketa na, nke kachasị mkpa, ntinye apoptosis na mkpụrụ ndụ kansa. LDC000067 na-egbochi ndenye P-TEFb dabere na in vitro. Na-ebute apoptosis in vitro na in vivo yana BI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A bụ onye na-egbochi CDK8 dị ike ma họrọ nke na-arụ ọrụ na sel AML nwere ọkwa dị elu nke serine phosphorylation nke STAT1 na STAT5 ngalaba transactivation. EL120-34A na-egbochi phosphorylation nke STAT1 S727 na STAT5 S726 na mkpụrụ ndụ kansa na vitro. N'oge niile, a hụla ụkpụrụ nke STATs- na NUP98-HOXA9-edegharị ederede dabere dị ka usoro kachasị eme ihe na vivo. |
| CPDB1540 | MSC2530818 | MSC2530818 bụ onye nwere ike, Nhọrọ, na Oral Bioavailable CDK8 Inhibitor nwere CDK8 IC50 = 2.6 nM; PK amụma mmadụ: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F> 75% |
| CPDB1574 | CYC-065 | CYC065 bụ ọgbọ nke abụọ, onye na-emechi ọnụ ATP-asọmpi nke CDK2/CDK9 kinase nwere ike antineoplastic na chemoprotective. |
| CPDB1594 | THZ531 | THZ531 bụ ihe mgbochi CDK12 na CDK13 covalent inhibitor. Kinases nke dabere na cyclin 12 na 13 (CDK12 na CDK13) na-arụ ọrụ dị oke egwu na nhazi nke ederede mkpụrụ ndụ ihe nketa. |
| CPDB1587 | THZ2 | THZ2, ihe analog nke THZ1, nke nwere ike ịgwọ ọrịa cancer ara na-adịghị mma (TNBC), ọ bụ ihe mgbochi CDK7 dị ike ma họrọ nke na-emeri nkwụsị nke THZ1 na vivo. IC50: CDK7= 13.9 nM; Mkpụrụ ndụ TNBC = 10 nM |
