Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
56 Results for "
CDK9 degrader
" in MedChemExpress (MCE) Product Catalog:
Products (56)
56 Results for "CDK9 degrader" in MCE Product Catalog:
10
10 Publications Verification
THAL-SNS-032 is a selective CDK9 PROTAC degrader. THAL-SNS-032 recruits CRBN to form a ternary complex with CDK9, thereby triggering ubiquitination and proteasomal degradation of CDK9. THAL-SNS-032 also induces the degradation of CDK1, CDK2 and CDK7. THAL-SNS-032 elevates pH2AX levels, reduces MCL1s expression, and activates caspase-3. THAL-SNS-032 induces cancer cell apoptosis, regulates transcription, and inhibits the replication of human cytomegalovirus (CMV) and SARS-CoV-2. THAL-SNS-032 can be used in research related to breast cancer, leukemia, cytomegalovirus infection and SARS-CoV-2 infection .
2
1
Target:
Research Areas:
(R)-CR8, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect . (R)-CR8 acts as a molecular glue degrader that depletes cyclin K .
1
1 Cited Publications
TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM) .
1
1 Cited Publications
Cat. No.: HY-162706
CAS No.: 2519823-37-9
BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer .
1
1 Cited Publications
Cat. No.: HY-18340A
CAS No.: 1786438-30-9
Synonyms: CR8, (R)-Isomer trihydrochloride
Target:
Research Areas:
(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect . (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K .
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand .
Cat. No.: HY-173523
CAS No.: 3054009-82-1
KI-CDK9d-32 is a selective CDK9 PROTAC degrader (IC50 = 3 nM; DC50 = 0.89 nM). KI-CDK9d-32 induces CDK9 degradation via the ubiquitin-proteasome pathway to abrogates CDK9 enzymatic and scaffolding functions, downregulates MYC expression and MYC-dependent signaling, represses TNF-alpha signaling pathways activity and pre-rRNA levels. KI-CDK9d-32 disrupts nucleolar homeostasis, blocks cell cycle progression and cellular translation by reducing 4EBP1 phosphorylation, and elicits cancer cell cytotoxicity in a CRBN-dependent manner, while high ABCB1 activity attenuates the efficacy. KI-CDK9d-32 can be used for the research of acute lymphoblastic leukemia, rhabdomyosarcoma, pancreatic adenocarcinoma .
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1 .
Cat. No.: HY-168518
CAS No.: 3117192-80-7
Target:
Research Areas:
PROTAC CDK9 degrader-9 is an orally active, selective CDK9 PROTAC degrader with a DC50 of 3.94 nM. PROTAC CDK9 degrader-9 downregulates downstream targets c-Myc and MCL-1. PROTAC CDK9 degrader-9 inhibits the proliferation of breast cancer cells. PROTAC CDK9 degrader-9 can be used for the research of triple-negative breast cancer .
Cat. No.: HY-178861
Target:
Research Areas:
dCDK9-202 is a CDK9 PROTAC degrader with a DC50 of 3.5 nM. dCDK9-202 induces CDK9 degradation via the ubiquitin-proteasome system. dCDK9-202 inhibits the growth of cancer cells in vitro and suppresses tumor growth in mouse xenograft models. dCDK9-202 is applicable for cancer-related research .
PROTAC CDK9 degrader-4 is a selective PROTAC CDK9 degrader. PROTAC CDK9 degrader-4 exhibits antiproliferative, pro-apoptotic and in vivo tumor growth inhibitory activities. PROTAC CDK9 degrader-4 can be used for the research of triple-negative breast cancer .
Cat. No.: HY-170978
CAS No.: 3039540-19-4
PROTAC CDK9 degrader-11 is an orally active, selective CDK9 PROTAC degrader with a DC50 of 1.09 nM. PROTAC CDK9 degrader-11 recruits CRBN to form a ternary complex and degrades CDK9 via the ubiquitin-proteasome pathway, thereby inhibiting RNA polymerase II phosphorylation and downregulating the expression of anti-apoptotic and pro-oncogenic genes, ultimately inducing apoptosis. PROTAC CDK9 degrader-11 is suitable for research on small-cell lung cancer (SCLC) .
Cat. No.: HY-155218
CAS No.: 2488892-09-5
TMX-2172 is a selective bivalent cereblon-recruiting PROTAC-based dual CDK2 and CDK5 degrader with IC50 values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer .
Cat. No.: HY-156084
CAS No.: 2809353-52-2
LL-K9-3 is a selective CDK9-cyclin T1 HyT degrader, with DC50 values of 0.662 μM and 0.589 μM for CDK9 and Cyclin T1, respectively. LL-K9-3 lacks an E3 ligand moiety and induces polyubiquitination and proteasome-mediated synchronous degradation of CDK9 and cyclin T1 via a hydrophobic tag-mediated mechanism. LL-K9-3 downregulates the protein levels of androgen receptor (AR) and c-Myc, and exhibits antiproliferative and pro-apoptotic (apoptosis) activity in prostate cancer cells. LL-K9-3 can be used in studies related to prostate cancer .
Cat. No.: HY-149962
CAS No.: 2935587-89-4
PROTAC CDK9 degrader-5 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-5 mediates CDK9 degradation via the proteasome. PROTAC CDK9 degrader-5 degrades CDK9 with DC50s of 0.10 μM and 0.14 μM for the CDK942 and CDK955 isoforms, respectively .
Cat. No.: HY-176451
CDK9 degrader-1 (Compound AZ-9) is a selective CDK9 degrader (DC50: 0.4073 µM). CDK9 degrader-1 recruits ATG101 to initiate the autophagy-lysosome pathway and forms autophagosomes by recruiting LC3, which then fuses with lysosomes to degrade CDK9 and its partner protein Cyclin T1 (DC50: 1.215 µM). CDK9 degrader-1 induces caspase 3-mediated apoptosis. CDK9 degrader-1 has antitumor activity in a mouse HCT116 xenograft model .
Cat. No.: HY-168896
CAS No.: 3066836-42-5
CDK9 autophagic degrader 1 (Compound 28) is a ATTEC degrader that can be used to degrade CDK9 and also affects the levels of the associated Cyclin T1. CDK9 autophagic degrader 1 shows over 80% CDK9 inhibition rate at 100 nM . ( Pink: LC3B ligand (HY-168897); Black: linker (HY-W017758); Blue: target protein ligand (HY-10008); linker + target protein ligand (HY-168898))
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
