| CAT # | Sunan samfur | Bayani |
| Saukewa: CPD100904 | Voruciclib | Voruciclib, wanda kuma aka sani da P1446A-05, shine mai hana furotin kinase na musamman don kinase 4 (CDK4) mai dogara da cyclin tare da yiwuwar aikin antineoplastic. CDK4 inhibitor P1446A-05 musamman yana hana CDK4-matsakaici G1-S lokaci mika mulki, kama hawan keke da kuma hana ciwon daji girma. Ana samun serine / threonine kinase CDK4 a cikin hadaddun tare da nau'in D-type G1 cyclins kuma shine kinase na farko don kunnawa akan haɓakar mitogenic, sakin sel daga matakin quiescent zuwa matakin hawan keke na G1 / S; CDK-cyclin complexes an nuna su phosphorylate da retinoblastoma (Rb) transcription factor a farkon G1, murkushe histone deacetylase (HDAC) da kuma toshe transcriptional danniya. |
| Saukewa: CPD100905 | Alvocidib | Alvocidib wani abu ne na roba N-methylpiperidinyl chlorophenyl flavone fili. A matsayin mai hana cyclin-dogara kinase, alvocidib yana haifar da kamawar kwayar halitta ta hanyar hana phosphorylation na cyclin-dependent kinases (CDKs) da kuma ta hanyar ƙaddamar da cyclin D1 da D3 magana, wanda ya haifar da kama G1 cell cycle da apoptosis. Wannan wakili kuma mai gasa ne mai hana aikin adenosine triphosphate. Bincika gwaje-gwajen asibiti masu aiki ko rufaffiyar gwajin asibiti ta amfani da wannan wakili. |
| Saukewa: CPD100906 | BS-181 | BS-181 babban zaɓi ne mai hana CDK don CDK7 tare da IC(50) na 21 nmol/L. Gwajin wasu CDKs da kuma wani 69 kinases ya nuna cewa BS-181 kawai ya hana CDK2 a matakan ƙasa da 1 micromol/L, tare da hana CDK2 35-ninka ƙasa da ƙarfi (IC(50) 880 nmol/L) fiye da CDK7. A cikin sel na MCF-7, BS-181 ya hana phosphorylation na CDK7 substrates, inganta tsarin sake zagayowar cell da apoptosis don hana ci gaban ƙwayoyin cutar kansa, kuma ya nuna tasirin antitumor a cikin vivo. |
| Saukewa: CPD100907 | Riviciclib | Riviciclib, wanda kuma aka sani da P276-00, shine mai hana flavone da cyclin kinase (CDK) mai hanawa tare da yiwuwar aikin antineoplastic. P276-00 zaɓaɓɓen ɗaure da kuma hana Cdk4/cyclin D1, Cdk1/cyclin B da Cdk9/cyclin T1, serine/threonine kinases waɗanda ke taka muhimmiyar rawa a cikin ka'idar tsarin tantanin halitta da haɓakar salula. Hana waɗannan kinases yana haifar da kamawar ƙwayar ƙwayar cuta a lokacin canjin G1/S, wanda hakan zai haifar da ƙaddamar da apoptosis, da kuma hana yaduwar ƙwayar ƙwayar cuta. |
| Saukewa: CPD100908 | Saukewa: MC180295 | MC180295 mai hanawa CDK9 ne mai zaɓin zaɓi (IC50 = 5 nM). (MC180295 yana da faffadan aikin rigakafin ciwon daji a cikin vitro kuma yana da tasiri a cikin nau'ikan ciwon daji na vivo. Bugu da ƙari, hana CDK9 yana da hankali ga mai hanawa na rigakafi α-PD-1 a cikin vivo, yana mai da shi kyakkyawan manufa don maganin ciwon daji na epigenetic. |
| 1073485-20-7 | Saukewa: LDC000067 | LDC000067 mai ƙarfi ne kuma mai hanawa CDK9. LDC000067 an hana rubutun in vitro a cikin gasa-ATP da kuma dogaro da kashi. Bayyanar bayanan kwayoyin halitta na sel da aka bi da su tare da LDC000067 sun nuna raguwar zaɓi na mRNAs na ɗan gajeren lokaci, gami da mahimman masu kula da yaduwa da apoptosis. Binciken hadawar de novo RNA ya ba da shawarar faffadan ingantacciyar rawar CDK9. A matakin kwayoyin halitta da salon salula, LDC000067 ya haifar da tasirin halayen halayen hana CDK9 kamar ingantaccen dakatarwar RNA polymerase II akan kwayoyin halitta kuma, mafi mahimmanci, shigar da apoptosis a cikin ƙwayoyin kansa. LDC000067 yana hana P-TEFb-dogara a rubutun in vitro. Yana haifar da apoptosis a cikin vitro da in vivo a hade tare da BI 894999. |
| Saukewa: CPD100910 | Saukewa: SEL120-34A | SEL120-34A shine mai hanawa CDK8 mai ƙarfi da zaɓi mai aiki a cikin sel AML tare da manyan matakan serine phosphorylation na STAT1 da STAT5 yankuna transactivation. EL120-34A yana hana phosphorylation na STAT1 S727 da STAT5 S726 a cikin ƙwayoyin ciwon daji a cikin vitro. A koyaushe, an lura da ƙa'idodin STATs- da NUP98-HOXA9- masu dogaro da rubutun a matsayin babban tsarin aiki a vivo. |
| Saukewa: CPDB1540 | Saukewa: MSC2530818 | MSC2530818 Mai Iko ne, Zaɓaɓɓe, da Mai hana CDK8 na Baka tare da CDK8 IC50 = 2.6 nM; Hasashen PK na ɗan adam: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F> 75%. |
| Saukewa: CPDB1574 | CYC-065 | CYC065 shine ƙarni na biyu, mai hanawa mai hanawa ATP da baki na CDK2/CDK9 kinase tare da yuwuwar ayyukan antineoplastic da chemoprotective. |
| Saukewa: CPDB1594 | THZ531 | THZ531 mai haɗakarwa CDK12 da CDK13 mai hanawa. Kinases masu dogaro da Cyclin 12 da 13 (CDK12 da CDK13) suna taka rawa mai mahimmanci a cikin tsarin kwafin kwayoyin halitta. |
| Saukewa: CPDB1587 | THZ2 | THZ2, analog na THZ1, tare da yuwuwar magance cutar kansar nono sau uku (TNBC), yana da ƙarfi kuma mai zaɓi CDK7 inhibitor wanda ke shawo kan rashin zaman lafiyar THZ1 a cikin vivo. IC50: CDK7= 13.9 nM; Kwayoyin TNBC = 10 nM |
