| Ologbo # | Orukọ ọja | Apejuwe |
| CPD100904 | Voruciclib | Voruciclib, ti a tun mọ ni P1446A-05, jẹ amuaradagba kinase inhibitor kan pato fun kinase ti o gbẹkẹle cyclin 4 (CDK4) pẹlu iṣẹ-ṣiṣe antineoplastic ti o pọju. CDK4 inhibitor P1446A-05 ni pato ṣe idiwọ CDK4-mediated G1-S alakoso iyipada, mimu gigun kẹkẹ sẹẹli ati idilọwọ idagbasoke sẹẹli alakan. Serine / threonine kinase CDK4 ni a ri ni eka kan pẹlu D-type G1 cycins ati ki o jẹ akọkọ kinase lati di mu ṣiṣẹ lori mitogenic fọwọkan, dasile awọn sẹẹli lati ipele quiescent sinu ipele gigun kẹkẹ G1 / S idagbasoke; Awọn eka CDK-cyclin ti han lati phosphorylate awọn retinoblastoma (Rb) ifosiwewe transcription ni kutukutu G1, nipo histone deacetylase (HDAC) ati idilọwọ ifasilẹ transcriptional. |
| CPD100905 | Alvocidib | Alvocidib jẹ agbo N-methylpiperidinyl chlorophenyl flavone sintetiki. Gẹgẹbi oludena ti kinase ti o gbẹkẹle cyclin, alvocidib nfa imudani ọmọ inu sẹẹli nipasẹ idilọwọ phosphorylation ti awọn kinases ti o gbẹkẹle cyclin (CDKs) ati nipasẹ ilana ilana cyclin D1 ati D3 ikosile, ti o mu ki G1 cell cycle arrest ati apoptosis. Aṣoju yii tun jẹ oludena ifigagbaga ti iṣẹ ṣiṣe triphosphate adenosine. Ṣayẹwo fun awọn idanwo ile-iwosan ti nṣiṣe lọwọ tabi awọn idanwo ile-iwosan pipade ni lilo aṣoju yii. |
| CPD100906 | BS-181 | BS-181 jẹ oludaniloju CDK ti o yan pupọ fun CDK7 pẹlu IC (50) ti 21 nmol/L. Idanwo awọn CDK miiran ati awọn kinases 69 miiran fihan pe BS-181 nikan ni idinamọ CDK2 ni awọn ifọkansi ti o kere ju 1 micromol/L, pẹlu CDK2 ni idinamọ 35-fold kere si agbara (IC(50) 880 nmol/L) ju CDK7. Ninu awọn sẹẹli MCF-7, BS-181 ṣe idiwọ phosphorylation ti awọn sobusitireti CDK7, igbega imudani ọmọ sẹẹli ati apoptosis lati ṣe idiwọ idagba awọn laini sẹẹli alakan, ati ṣafihan awọn ipa antitumor ni vivo. |
| CPD100907 | Riviciclib | Riviciclib, ti a tun mọ ni P276-00, jẹ oludena flavone ati cyclin ti o gbẹkẹle kinase (CDK) pẹlu iṣẹ-ṣiṣe antineoplastic ti o pọju. P276-00 yiyan sopọ si ati ki o ṣe idiwọ Cdk4/cyclin D1, Cdk1/cyclin B ati Cdk9/cyclin T1, serine/threonine kinases ti o ṣe awọn ipa pataki ninu ilana ilana sẹẹli sẹẹli ati afikun cellular. Idinamọ ti awọn kinases wọnyi nyorisi imuni ọmọ inu sẹẹli lakoko iyipada G1/S, nitorinaa yori si ifakalẹ ti apoptosis, ati idinamọ ti ilọsiwaju sẹẹli tumo. |
| CPD100908 | MC180295 | MC180295 jẹ onidalẹkun CDK9 yiyan pupọ (IC50 = 5 nM). (MC180295 ni iṣẹ ṣiṣe egboogi-akàn gbooro ni fitiro ati pe o munadoko ninu awọn awoṣe akàn vivo. Ni afikun, idinamọ CDK9 ṣe ifarabalẹ si inhibitor checkpoint ajẹsara α-PD-1 ni vivo, ti o jẹ ki o jẹ ibi-afẹde ti o dara julọ fun itọju ailera akàn ti akàn. |
| 1073485-20-7 | LDC000067 | LDC000067 jẹ oludena CDK9 ti o lagbara ati yiyan. LDC000067 ni idinamọ in vitro transcription ni ATP-idije ati ọna ti o gbẹkẹle iwọn lilo. Isọjade ikosile jiini ti awọn sẹẹli ti a tọju pẹlu LDC000067 ṣe afihan idinku yiyan ti awọn mRNAs igba diẹ, pẹlu awọn olutọsọna pataki ti afikun ati apoptosis. Itupalẹ ti iṣelọpọ de novo RNA daba ipa rere jakejado ti CDK9. Ni ipele molikula ati cellular, LDC000067 awọn ipa ẹda ti o jẹ ihuwasi ti idinamọ CDK9 gẹgẹbi imudara imudara ti RNA polymerase II lori awọn Jiini ati, pataki julọ, ifakalẹ ti apoptosis ninu awọn sẹẹli alakan. LDC000067 ṣe idiwọ P-TEFb-igbẹkẹle in vitro transcription. Ṣe agbejade apoptosis in vitro ati in vivo ni apapo pẹlu BI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A jẹ oludaniloju CDK8 ti o lagbara ati yiyan ti nṣiṣe lọwọ ninu awọn sẹẹli AML pẹlu awọn ipele giga ti serine phosphorylation ti STAT1 ati awọn ibugbe transactivation STAT5. EL120-34A ṣe idiwọ phosphorylation ti STAT1 S727 ati STAT5 S726 ninu awọn sẹẹli alakan ni fitiro. Ni igbagbogbo, ilana ti STATs- ati NUP98-HOXA9-kikọsilẹ ti o gbẹkẹle ni a ti ṣakiyesi bi ilana iṣe ti o ga julọ ni vivo. |
| CPDB1540 | MSC2530818 | MSC2530818 jẹ Agbara, Yiyan, ati Orally Bioavailable CDK8 Inhibitor pẹlu CDK8 IC50 = 2.6 nM; Asọtẹlẹ PK eniyan: Cl ~ 0.14 L / H / Kg; t1/2 ~ 2.4h; F > 75%. |
| CPDB1574 | CYC-065 | CYC065 jẹ iran-keji, inhibitor ATP-ifigagbaga ti ẹnu-ọna ti CDK2/CDK9 kinases pẹlu agbara antineoplastic ati awọn iṣẹ ṣiṣe chemoprotective. |
| CPDB1594 | THZ531 | THZ531 jẹ CDK12 kovalent ati inhibitor covalent CDK13. Kinases ti o gbẹkẹle cyclin 12 ati 13 (CDK12 ati CDK13) ṣe awọn ipa to ṣe pataki ni ilana ti transcription pupọ. |
| CPDB1587 | THZ2 | THZ2, afọwọṣe ti THZ1, pẹlu agbara lati tọju akàn igbaya igbaya Mẹta-odi (TNBC), o jẹ oludaniloju CDK7 ti o lagbara ati ti o yan eyi ti o bori aiṣedeede ti THZ1 ni vivo. IC50: CDK7 = 13.9 nM; Awọn sẹẹli TNBC = 10 nM |
