| CAT # | Izina ryibicuruzwa | Ibisobanuro |
| CPD100904 | Voruciclib | Voruciclib, izwi kandi nka P1446A-05, ni poroteyine ya kinase inhibitor yihariye ya kinase iterwa na kinase 4 (CDK4) ifite ibikorwa bya antineoplastique. CDK4 inhibitor P1446A-05 irabuza cyane cyane CDK4 yunganirwa na G1-S icyiciro cya kabiri, gufata amagare ya selile no kubuza gukura kwa kanseri. Serine / threonine kinase CDK4 iboneka murwego rufite D-G1 yo mu bwoko bwa G1 kandi niyo kinase ya mbere yatangiye gukora nyuma yo gukanguka kwa mitogenic, ikarekura ingirabuzimafatizo kuva mukanya gato ikagera kuri G1 / S. CDK-cyclin yerekanwe kuri fosifora yibintu byandikirwa retinoblastoma (Rb) mugitangiriro cya G1, ikuraho histone deacetylase (HDAC) no guhagarika gukandamizwa. |
| CPD100905 | Alvocidib | Alvocidib ni synthique N-methylpiperidinyl chlorophenyl flavone. Nkumwanya wa kinase iterwa na cyclin, alvocidib itera gufatwa kwingirangingo mu gukumira fosifora ya kinase iterwa na cyclin (CDKs) ndetse no kugabanya imvugo ya cyclin D1 na D3, bigatuma G1 itabwa muri yombi na apoptose. Iyi agent nayo irwanya irushanwa ryibikorwa bya adenosine triphosphate. Reba ibizamini bya clinique ikora cyangwa ibizamini bya clinique bifunze ukoresheje iyi agent. |
| CPD100906 | BS-181 | BS-181 ni CDK itoranya cyane ya CDK7 hamwe na IC (50) ya 21 nmol / L. Igeragezwa ryizindi CDK kimwe nizindi kinase 69 zerekanye ko BS-181 yabujije CDK2 gusa yibitekerezo biri munsi ya micromol / L, CDK2 ikabuzwa inshuro 35 imbaraga nke (IC (50) 880 nmol / L) kuruta CDK7. Muri selile MCF-7, BS-181 yabujije fosifora ya CDK7 insimburangingo, iteza imbere ifatwa ry’ingirabuzimafatizo na apoptose kugira ngo ibuze imikurire ya kanseri ya kanseri, kandi yerekana ingaruka za antitumor muri vivo. |
| CPD100907 | Riviciclib | Riviciclib, izwi kandi nka P276-00, ni flavone na cyclin biterwa na kinase (CDK) inhibitor hamwe nibikorwa bya antineoplastique. P276-00 guhitamo guhuza no kubuza Cdk4 / cyclin D1, Cdk1 / cyclin B na Cdk9 / cyclin T1, serine / threonine kinase igira uruhare runini mugutunganya ingirabuzimafatizo no gukwirakwiza selile. Kubuza izo kinase biganisha ku gufatwa kwingirangingo mugihe cyinzibacyuho ya G1 / S, bityo bigatuma habaho kwinjiza apoptose, no kubuza ikwirakwizwa rya selile. |
| CPD100908 | MC180295 | MC180295 ni CDK9 ihitamo cyane (IC50 = 5 nM). . |
| 1073485-20-7 | LDC000067 | LDC000067 ninzitizi ikomeye kandi itoranya CDK9. LDC000067 yabujijwe kwandukura vitro muburyo bwa ATP-irushanwa kandi ikabije. Imvugo yerekana imiterere ya selile zavuwe na LDC000067 yerekanaga igabanuka ryatoranijwe rya mRNAs zimara igihe gito, harimo nubugenzuzi bukomeye bwo gukwirakwiza na apoptose. Isesengura rya de novo RNA synthesis ryagaragaje uruhare runini rwa CDK9. Ku rwego rwa molekuline na selile, LDC000067 yerekanye ingaruka ziranga CDK9 nko guhagarika ihagarikwa rya RNA polymerase II kuri gen, cyane cyane, kwinjiza apoptose mungirangingo za kanseri. LDC000067 ibuza P-TEFb iterwa na transcription. Itera apoptose muri vitro no muri vivo ifatanije na BI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A ninzitizi ikomeye kandi yatoranijwe ya CDK8 ikora muri selile ya AML ifite urwego rwo hejuru rwa fosifora ya serine ya STAT1 na STAT5 transactivation. EL120-34A ibuza fosifora ya STAT1 S727 na STAT5 S726 muri selile ya kanseri muri vitro. Mubisanzwe, amabwiriza ya STATs- na NUP98-HOXA9- kwandukura byaragaragaye nkuburyo bwiganje bwibikorwa muri vivo. |
| CPDB1540 | MSC2530818 | MSC2530818 ni Imbaraga, Guhitamo, no Muburyo Bioavailable CDK8 Inhibitor hamwe na CDK8 IC50 = 2.6 nM; Ubuhanuzi bwa PK bwabantu: Cl ~ 0.14 L / H / Kg; t1 / 2 ~ 2.4h; F> 75%. |
| CPDB1574 | CYC-065 | CYC065 ni igisekuru cya kabiri, kiboneka mu magambo ATP irushanwa irwanya CDK2 / CDK9 kinase hamwe nibikorwa bya antineoplastique na chemoprotective. |
| CPDB1594 | THZ531 | THZ531 ni covalent CDK12 na CDK13 ya covalent inhibitor. Cyclin-iterwa na kinase 12 na 13 (CDK12 na CDK13) bigira uruhare runini mugutunganya transcription. |
| CPDB1587 | THZ2 | THZ2, igereranya na THZ1, ifite ubushobozi bwo kuvura kanseri y'ibere ya gatatu-mbi (TNBC), ni inhibitor ikomeye kandi itoranya CDK7 inesha ihungabana rya THZ1 muri vivo. IC50: CDK7 = 13.9 nM; TNBC selile = 10 nM |
