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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
426 Results for "
cdk2
" in MedChemExpress (MCE) Product Catalog:
Products (426)
426 Results for "cdk2" in MCE Product Catalog:
Cat. No.: HY-162802
PI3K/AKT-IN-4 (compound 3) is a diterpenoid that can be isolated from the roots and rhizomes of Salvia castanea Dielsf. PI3K/AKT-IN-4 has antitumor activity, inhibiting cell viability and proliferation (IC50=4.72 μM) and promoting apoptosis by blocking the G0/G1 phase of the Hep3B cell cycle, inducing mitochondrial dysfunction and oxidative stress. In addition, PI3K/AKT-IN-4 inhibits hepatocellular carcinoma by inhibiting the PI3K-Akt signaling pathway and binding to PARP1 and CDK2 targets .
Cat. No.: HY-181838
CAS No.: 3064485-73-7
CIRc-014 is an orally active Cyclin A/B inhibitor with a Cyclin A IC50 of 0.05 μM, Cyclin A Kd of 2.7 nM, Cyclin B IC50 of less than 0.02 μM and Cyclin B Kd of 1.0 nM. CIRc-014 activates the spindle assembly checkpoint and promotes the formation of a complex between Cyclin B and CDK2 by blocking the RxL interaction of Cyclin A/B. CIRc-014 can induce replication stress, DNA damage, mitotic arrest and apoptosis in tumor cells. CIRc-014 showed tumor growth inhibition and regression in NCI-H69 and NCI-H446 small cell lung cancer xenograft models. CIRc-014 can be used for the research of small-cell lung cancer [2].
Cat. No.: HY-183070
CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC50 of 0.88 nM. CXJ2080 recruits VHL E3 ligase to induce ubiquitin-proteasome-dependent CDK7 degradation, disrupts the CDK7-cyclin H-MAT1 complex, suppresses CDK7-dependent phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. CXJ2080 activates the p53-p21 axis, suppresses MYC-driven signaling, induces leukemia cell cycle arrest, apoptosis, and differentiation, reduces CD117 expression, spares platelets and normal PBMCs, maintains sustained CDK7 degradation post-washout. CXJ2080 can be used for the research of acute leukemia .
Cat. No.: HY-183456
CAS No.: 71308-35-5
Research Areas:
Tyrphostin AG17 is an orally active CDK2 inhibitor and EGFR tyrosine kinase antagonist. Tyrphostin AG17 reduces the levels of p21 and p16. Tyrphostin AG17 induces G1 phase cell cycle arrest, Apoptosis, mitochondrial dysfunction, decreased ATP levels, and inhibits DNA, RNA and protein synthesis, adipogenesis, and lipid synthesis. Tyrphostin AG17 inhibits fat accumulation, white adipose tissue hypertrophy, and alterations of glycogen and lipid inclusions in hepatocytes in obese mice without changing their serum biochemical parameters. Tyrphostin AG17 exhibits anticancer effects. Tyrphostin AG17 can be used in research related to immunoblastic lymphoma, leukemia, ovarian cancer, glioblastoma, colon cancer, breast cancer, melanoma, obesity and hepatic steatosis [2] .
Cat. No.: HY-116054
CAS No.: 1314096-68-8
Research Areas:
Ibulocydine is an isobutyrate prodrug of the Cdk inhibitor BMK-Y101 (HY-188159), with oral activity, and exhibits IC50 values of approximately 50 nM against CDK1/CDK2, 530 nM against CDK7/cyclin H/Mat1, and 85 nM against CDK9/cyclin T. Ibulocydine reduces the phosphorylation levels of Rb, nucleolin, and RNA polymerase II CTD Ser-5 and Ser-2, downregulates the expression of Mcl-1, survivin, and XIAP, decreases MMP-9 expression, and lowers the Bcl-2/Bax ratio, activates calpain-mediated Bax cleavage, cytochrome c release, and caspase activation. Ibulocydine induces apoptosis, inhibits the growth of cancer cells and xenografts, enhances the sensitivity of cancer cells to TRAIL and radiotherapy, and blocks cancer cell metastasis. Ibulocydine can be used in research related to various cancers, including hepatocellular carcinoma, triple-negative breast cancer, lung cancer, and colon cancer [2] .
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-173007
CAS No.: 3050831-84-7
Research Areas:
ALK/PI3K/AKT-IN-1 (Compound 45) inhibits the proliferation of cancer cell A549, H1975 and PC9 with an IC50 of 0.44, 0.83 and 1.51 μM. ALK/PI3K/AKT-IN-1 increases the expression of p21 and p27, inhibits the activity of CDK2 and p-Rb, arrests the cell cycle at G1 phase. ALK/PI3K/AKT-IN-1 inhibits the ALK/PI3K/AKT signaling pathway, promotes the depolarization of mitochondrial membrane potential, and inducing apoptosis in A549 cell. ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheroids .
Cat. No.: HY-187643
CAS No.: 304911-07-7
Research Areas:
CGC-11144 hydrochloride is a polyamine analog. CGC-11144 hydrochloride reduces the kinase activities of CDK4, CDK2 and CDK6, induces activation of the p53 pathway and p53-dependent p21 expression, and mediates cell cycle regulation, growth inhibition and apoptosis. CGC-11144 hydrochloride induces G1 phase cell cycle arrest, downregulates cyclin D1 and cyclin B1, upregulates cyclin E, induces dephosphorylation of pRb, and inhibits ERα-mediated transcriptional activity by disrupting the DNA binding of Sp1/Sp3 to the ERα promoter, while also stimulating activation of the JNK/AP-1 pathway. CGC-11144 hydrochloride can be used in research related to breast cancer, choroidal neovascularization and cancer [2] .
Cat. No.: HY-N8146
CAS No.: 53729-52-5
Cat. No.: HY-119715
CAS No.: 486414-35-1
Research Areas:
AG-012986 is a pan-CDK inhibitor with Ki values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces Ki-67 expression. AG-012986 exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity [2] .
Cat. No.: HY-182470
CAS No.: 486414-32-8
Target:
AG-012986 (dihydrochloride) is a pan-CDK inhibitor with Ki values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 (dihydrochloride) causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 (dihydrochloride) induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces Ki-67 expression. AG-012986 (dihydrochloride) exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 (dihydrochloride) can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity [2] .
Cat. No.: HY-183273
CAS No.: 3087270-50-3
BRD4/AKT-IN-1 is a BRD4/AKT inhibitor with BRD4 IC50 66.12 nM and AKT1 IC50 143.81 nM. BRD4/AKT-IN-1 blocks BRD4-mediated c-Myc transcriptional regulation, modulates AKT1 signaling, decouples AKT phosphorylation from pro-survival effectors. BRD4/AKT-IN-1 induces G0/G1 cell cycle arrest via downregulated phosphorylated RB, cyclin E1, CDK2. BRD4/AKT-IN-1 elevates LC3B levels to promote autophagy. BRD4/AKT-IN-1 promotes apoptosis in cancer cells. BRD4/AKT-IN-1 can be used for the research of metastatic castration-resistant prostate cancer .
Target:
PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1 SnRK
Research Areas:
RSS0680 is a small noncoding RNA (sRNA) targeting the mRNA ribosome binding site (RBS) and a PROTAC. RSS0680 competitively binds to RBS through the conserved CCUCCUCCC anti-Shine-Dalgarno (aSD) sequence and inhibits the translation initiation of target genes. RSS0680 can interact with the DUF1127 protein CcaF1, regulate its own stability and participate in bacterial oxidative stress defense, enhancing the host's resistance to heat shock and oxidative damage by affecting pathways such as C1 metabolism and pyruvate dehydrogenase complex. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used to study diseases or disorders mediated by aberrant kinase activity and regulatory mechanisms of noncoding RNAs in α-proteobacteria[1][2].
Cat. No.: HY-W097625R
CAS No.: 26964-24-9
Cat. No.: HY-181906
Target:
Research Areas:
ZnPc-PEG2-VH032 is a VHL-pathway-dependent photodegradation targeting chimera (PDTAC) and cytotoxic agent. ZnPc-PEG2-VH032 (HY-120217) binds to the VHL ligand domain, and then specifically degrades VHL under light irradiation, a process independent of non-specific ROS-mediated protein damage. ZnPc-PEG2-VH032 uses Zinc phthalocyanine (HY-19204) as a photosensitizer, and generates ROS via type I and type II photodynamic pathways under 680 nm LED irradiation. On one hand, it targets and degrades the bound VHL protein through ROS; on the other hand, it exerts direct photodynamic cytotoxicity. Meanwhile, the degradation of VHL downregulates the phosphorylation level of CDK2/4, induces cell cycle arrest in tumor cells, further enhances the sensitivity of tumor cells to oxidative damage caused by ROS, and achieves a synergistic anti-tumor effect. ZnPc-PEG2-VH032 exerts significant in vivo efficacy in an orthotopic mouse model of non-muscle invasive bladder cancer (NMIBC) .
Cat. No.: HY-170820
CAS No.: 3006788-11-7
Target:
Molecular Glues Eukaryotic Release Factor (eRF) Bcl-2 Family CDK EGFR HSP Androgen Receptor c-Myc
Research Areas:
XYD049 is a CRBN-based molecular glue degrader targeting GSPT1, with a DC50 of 19 nM. XYD049 mediates the formation of a ternary complex between CRBN and GSPT1, thereby triggering CRBN- and proteasome-dependent degradation of GSPT1. By degrading GSPT1, XYD049 downregulates castration-resistant prostate cancer (CRPC)-related oncogenes, including BCL2, CDK2, E2F3, EGFR, HSP90B1, TMPRSS2, AR, AR-V7, PSA and c-Myc. XYD049 inhibits cancer cell growth and suppresses tumor growth in mice. XYD049 can be used for research on castration-resistant prostate cancer. XYD049 consists of a linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-based E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), among which the E3 ligase ligand plus linker forms the conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .
Cat. No.: HY-P811831
Synonyms: Cyclin-dependent kinase 2-interacting protein, cdk2-interacting protein, CINP
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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
