Search Result
Results for "
G0/G1 phase
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-13680
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Dian III; N-Methylisoindigotin; Natura-α
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Apoptosis
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Cancer
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Meisoindigo (Dian III), a derivative of Indirubin (HY-N0117), halts the cell cycle at the G0/G1 phase and induces apoptosis in primary acute myeloid leukemia (AML) cells. Meisoindigo exhibits high antitumor activity .
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- HY-152245
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Epigenetic Reader Domain
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Cancer
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Physachenolide C is a potent and selective BET inhibitor that induces apoptosis and arrests the cell cycle in the G0-G1 phase, with antitumor activity .
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- HY-124261
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Apoptosis
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Cancer
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Sampangine is an alkaloid that induces apoptosis by inducing cell cycle arrest in the G0/G1 phase. Sampangine can inhibit the biosynthesis of heme .
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- HY-155552
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Apoptosis
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Cancer
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GSPT1 degrader-1 (compound 9q) is a potent degrader of G1 to S phase transition 1 (GSPT1) via ubiquitin-proteasome system. GSPT1 degrader-1 also induces cell G0/G1 phase arrest and apoptosis .
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- HY-13768C
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SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate
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Topoisomerase
Apoptosis
Autophagy
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Cancer
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Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity .
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- HY-13768
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SKF 104864A; NSC 609669
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Topoisomerase
Autophagy
Apoptosis
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Cancer
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Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity .
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- HY-162416
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CDK
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Cancer
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CDK7-IN-27 (Compound 37) is a selective inhibitor for cyclin-dependent kinase 7 (CDK7), with Ki of 3 nM. CDK7-IN-27 arrests the cell cycle at G0/G1 phase .
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- HY-155544
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c-Met/HGFR
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Cancer
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Antitumor agent-111 (compound 46) is an c-Met kinase inhibitor (IC50=46 nM) with antitumor and antiproliferative activity. Antitumor agent-111 arrests cell cycle at G0/G1 phase, and induces apoptosis .
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- HY-155503
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Apoptosis
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Cancer
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Antitumor agent-103 (compound 24l) is an apoptosis inducer with antiproliferative and anti-clony formation activities. Antitumor agent-103 arrests cell cycle at G0/G1 phase, enhances NO production, and exhibits anti-tumor activity .
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- HY-147801
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Topoisomerase
Apoptosis
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Cancer
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Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis .
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- HY-145762
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Apoptosis
Histone Methyltransferase
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Cancer
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YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma .
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- HY-149063
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Apoptosis
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Cancer
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Antitumor agent-92, an Icaritin (HY-N0678) derivative, causes arrest at the G0/G1 phase in the cell cycle and induces cell apoptosis. Antitumor agent-92 has the potential for hepatocellular carcinoma (HCC) research .
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- HY-144733
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Estrogen Receptor/ERR
Apoptosis
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Cancer
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ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells .
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- HY-163722
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EGFR
Dihydrofolate reductase (DHFR)
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Cancer
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EGFR/DHFR-IN-1 (Compound 10e) is a dual inhibitor of EGFR and DHFR with IC50s of 0.151 and 0.541 µM, respectively. EGFR/DHFR-IN-1 arrests the cell cycle at both G0-G1 and S phases .
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- HY-159096
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Apoptosis
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Cancer
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Apoptosis inducer 21 (Compound 5h) inhibits the proliferation of lung cancer cell H69AR with an IC50 of 1.58 μM. Apoptosis inducer 21 arrests the cell cycle at G0/G1 phase, induces apoptosis in H69AR .
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- HY-146063
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Apoptosis
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Cancer
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Anticancer agent 54 is a potent anticancer agent. Anticancer agent 54 shows antiproliferative activity. Anticancer agent 54 induces apoptosis and cell cycle arrest at G0/G1 phases. Anticancer agent 54 shows anticancer activity depends on DNA intercalation and ROS generation .
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- HY-146040
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Apoptosis
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Cancer
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Anticancer agent 47 (compound 4j) is a potent anticancer agent. Anticancer agent 47 shows antiproliferative activities. Anticancer agent 47 induces apoptosis and cell cycle arrest at G0/G1 phase. Anticancer agent 47 shows shows antitumor activities in vivo .
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- HY-10638
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c-Kit
Apoptosis
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Cancer
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AP23464 is an ATP-based inhibitor for Kit, that inhibits the phosphorylation of Kit wildtype and mutants, with IC50 of 5-85 nM. AP23464 inhibits the proliferation of Kit mutated cells (IC50 is 3-20 nM), arrests the cell cycle at G0/G1 phase, and induces apoptosis in Kit mutated cells .
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- HY-144394
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Apoptosis
c-Met/HGFR
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Cancer
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Antitumor agent-45 (Compound 21) could induce and stimulate A549 cells apoptosis in G0/G1 and G2/M phase. Antitumor agent-45 (Compound 21) inhibits c-Met expression to regulate the growth of tumor cells .
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- HY-W014940
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Reactive Oxygen Species
Apoptosis
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Others
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Ethylene glycol dimethacrylate is a methacrylate monomer, exhibits cytotoxic and genotoxic effects on human gingival fibroblasts (HGFs). Ethylene glycol dimethacrylate increases intracellular reactive oxygen species (ROS) production, causes DNA damage, increases apoptosis and causes cell cycle arrest in G1/G0 phase .
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- HY-129592
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Apoptosis
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Cancer
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p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cell cycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis .
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- HY-165064
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L-Erythro cer(d18:1/2:0); N-Acetyl-L-erythro-sphingosine; Acetyl-L-erythro-sphingosine
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Others
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Cancer
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C2 L-Erythro ceramide (d18:1/2:0) is a cell-permeable sphingolipid. C2 L-Erythro ceramide (d18:1/2:0) induces cell cycle arrest in the G0/G1 phase and inhibits cell growth .
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- HY-146203
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FAK
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Cancer
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Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase.
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- HY-143490
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PAK
Apoptosis
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Cancer
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PAK4-IN-2 is a highly potent PAK4 inhibitor with IC50 value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer .
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- HY-146445
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Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
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P300 bromodomain-IN-1 (Compoun 1u) is a potent p300 (EP300) bromodomain inhibitor with an IC50 of 49 nM. P300 bromodomain-IN-1 suppresses the expression of c-Myc and induces G1/G0 phase arrest and apoptosis in OPM-2 cells .
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- HY-N7844
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Benzyladenosine
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Apoptosis
Adenosine Receptor
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Inflammation/Immunology
Cancer
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N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma - .
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- HY-N1930
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Hinesol
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Apoptosis
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Cancer
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(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cell cycle arrest at G0/G1 phase. (-)-Hinesol downregulates MEK/ERK pathway and NF-κB pathway and mediates theexpression of cyclin D1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer .
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- HY-W747572
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(R)-(+)-perillyl alcohol
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Ras
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Cancer
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(+)-Perillyl alcohol is the enantiomer of S-(-)-Perillyl alcohol (HY-116514). (+)-Perillyl alcohol can inhibit the growth of polypeptides and block the cell cycle in the G0/G1 phase. (+)-Perillyl alcohol induces cell signaling that is associated with changes in cytoskeletal actin organization and reduced protein expression of growth regulatory proteins such as Ras and CDC2 kinase .
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- HY-159101
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EGFR
PD-1/PD-L1
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Cancer
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EP26 is a potent and orally active EGFR and PD-L1 inhibitor with IC50 values of 48.6 nM, 1.77 µM, respectively. EP26 decreased the protein expression of p-EGFR. EP26 induces cell cycle arrest at G0/G1 phase. EP26 has the potential for the research of glioblastoma .
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- HY-146132
-
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EGFR
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Cancer
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EGFR-IN-55 (Compound 8a) is a potent EGFR inhibitor with IC50 values of 70 nM and 3.9 nM against EGFR WT and EGFR L858R/T790M, respectively. EGFR-IN-55 arrests NCI-H1975 cells in G0/G1 phase and shows anticancer activity .
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- HY-17408
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-
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- HY-10815
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Sigma Receptor
Apoptosis
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Neurological Disease
Cancer
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σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells .
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- HY-120654
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Apoptosis
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Cancer
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[1,1′:4′,1′′-Terphenyl]-3,4′′,5-triol (compound 13g) is a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells. [1,1′:4′,1′′-Terphenyl]-3,4′′,5-triol shows a potent apoptotic effect .
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- HY-162755
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SHP2
Apoptosis
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Cancer
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SHP2-IN-30 (compound 14i) is an allosteric SHP2 inhibitor with an IC50 of 104 nM. SHP2-IN-30 shows low inhibitory effect on SHP2-PTP. SHP2-IN-30 induces cell apoptosis and arrests the cell cycle at the G0/G1 phase .
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- HY-149891
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HSP
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Cancer
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HSP90-IN-23 (Comp 12-1) is an inhibitor of heat shock protein 90(HSP90) with an IC50 of 9 nM. HSP90-IN-23 induces apoptosis of tumor cells and arrests the tumor cell cycle in G0/G1 phase. HSP90-IN-23 can be used for cancer research .
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- HY-N12044
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Apoptosis
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Cancer
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Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
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- HY-110293
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FLT3
Apoptosis
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Cancer
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CHMFL-FLT3-122 is a potent, selective and orally active FLT3 kinase with an IC50 of 40 nM. CHMFL-FLT3-122 shows selectivity for FLT3 over BTK (IC50 of 421 nM) and c-KIT (IC50 of 559 nM) kinases. CHMFL-FLT3-122 induces apoptosis by arresting the cell cycle into the G0/G1 phase .
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- HY-15221
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Apoptosis
Histone Demethylase
MDM-2/p53
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Cardiovascular Disease
Cancer
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Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis .
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- HY-149735
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Epigenetic Reader Domain
Apoptosis
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Cancer
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BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .
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- HY-122359A
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rel-L-Centchroman; Ormeloxifene
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Estrogen Receptor/ERR
Apoptosis
Reactive Oxygen Species
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Cancer
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rel-Levormeloxifene (rel-L-Centchroman) is the relative configuration of Levormeloxifene (HY-122359). rel-Levormeloxifene is a selective estrogen receptor modulator (SERM). rel-Levormeloxifene inhibits proliferation of leukemia cells with IC50 about 7 μM, arrests cell cycle at G0/G1 phase, and induces apoptosis. rel-Levormeloxifene induces differentation of myelogenesis leukemia, and enhances ROS production in K562 cells .
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- HY-162868
-
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c-Met/HGFR
HDAC
Apoptosis
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Cancer
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c-Met/HDAC-IN-4 is a dual inhibitor of c-Met/HDAC. The IC50 value of c-Met/HDAC-IN-4 for c-Met is 28.92 nM. c-Met/HDAC-IN-4 can induce G0/G1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells, and it inhibits the proliferation and invasion of breast cancer cell lines .
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- HY-156453
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PAK
Apoptosis
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Cancer
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PAK4-IN-3(compound 27e) is aPAK4inhibitor, with theIC50of 10 nM.PAK4-IN-3shows antiproliferative activity against A549 cells with anIC50value of 0.61μM, and inducesapoptosisof A549 cells in a concentration-dependent manner and blocked the cell cycle at phase G0/G1 .
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- HY-157814
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Apoptosis
Epigenetic Reader Domain
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Cancer
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Menin-MLL inhibitor-25 (compound A6) is a potent Menin-MLL interaction inhibitor with an IC50 value of 0.38 µM. Menin-MLL inhibitor-25 shows anti-proliferative activity. Menin-MLL inhibitor-25 induces apoptosis and cell cycle arrest at G0/G1 phase. Menin-MLL inhibitor-25 reverses the differentiation arrest .
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- HY-163535
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HDAC
DNA Methyltransferase
Apoptosis
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Inflammation/Immunology
Cancer
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J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs) .
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- HY-147935
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Akt
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Cancer
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NTQ1062 is a potent and orally active Akt inhibitor with IC50s of 0.4 nM, 6.3 nM and 0.1 nM for Akt1, Akt2 and Akt3, respectively. NTQ1062 induces cell apoptosis and arrests the cell cycle at G0/G1 phase. NTQ1062 exhibits antiproliferation activity against various cancer cells. NTQ1062 exhibits potent antitumor efficacy in LNCap xenograft mouse model .
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- HY-123486
-
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Apoptosis
Bcr-Abl
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Cancer
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HS-438 is a potent and selective BCR-ABL inhibitor. HS-438 shows antiproliferative activity. HS-438 decreases the expression of phosphorylation of BCR-ABL (Tyr177). HS-438 induces apoptosis and cell cycle arrest at G0/G1 phase. HS-438 shows antitumor activity. HS-438 has the potential for the research of chronic myeloid leukemia (CML) .
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- HY-15485
-
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Phosphodiesterase (PDE)
Apoptosis
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Inflammation/Immunology
Cancer
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Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma .
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- HY-114414
-
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HDAC
mTOR
Apoptosis
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Cancer
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HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies .
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- HY-151630
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Carbonic Anhydrase
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Cancer
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hCAIX-IN-16 (Compound 12d) is hCA IX inhibitor, with Ki values of 190.0 and 187.9 nM for hCA IX and hCA XII, respectively. hCAIX-IN-16 can arrest the cell cycle of breast cancer MDA-MB-468 in G0-G1 and S phase and induce apoptosis. hCAIX-IN-16 shows good broad-spectrum anticancer activity and can be used for cancer research .
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-
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- HY-155406
-
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Estrogen Receptor/ERR
Caspase
Bcl-2 Family
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Cancer
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Estrogen receptor modulator 10 (compound G-5b) is an Estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 can induce apoptosis. Estrogen receptor modulator 10 can block cells at the G1/G0 phase. Estrogen receptor modulator 10 can be used in cancer studies .
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- HY-17408R
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Compactin(Standard); ML236B (Standard)
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HMG-CoA Reductase (HMGCR)
Bacterial
Autophagy
Apoptosis
Antibiotic
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Infection
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
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Mevastatin (Standard) is the analytical standard of Mevastatin. This product is intended for research and analytical applications. Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment .
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- HY-159149
-
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Reactive Oxygen Species
Apoptosis
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Cancer
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Antitumor agent-182 (Compound 12a) decreases mitochondrial membrane potential (MMP) and enhances ROS levels. Antitumor agent-182 arrests the cell cycle at G0/G1 phase, induces apoptosis in HeLa. Antitumor agent-182 inhibits the proliferation of HeLa, PC-3 and HCT-15 with IC50s of 8.83, 10.07 and 7.84 μM, respectively .
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- HY-163894
-
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Apoptosis
HDAC
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Cancer
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HDAC6-IN-48 (compound 5i) is a potent and selective HDAC6 inhibitor with IC50 values of 5.16, 396.72, 638.08 nM for HDAC6, HDAC3, HDAC1, respectively. HDAC6-IN-48 induces apoptosis and cell cycle arrest at G0/G1 phase. HDAC6-IN-48 increases the protein expression of acetylated α-tubulin .
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- HY-N3764
-
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Akt
Dihydrofolate reductase (DHFR)
Endogenous Metabolite
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Others
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Diosbulbin C is a diterpene lactone component, which can be extracted from traditional Chinese medicine Dioscorea bulbifera L.. Diosbulbin C possesses high anticancer activity in non-small cell lung cancer (NSCLC). Diosbulbin C could induce cell cycle arrest at G0/G1 phase in NSCLC. Diosbulbin C also inhibits the proliferation of NSCLC cells, possibly by downregulating the expression/activation of AKT, DHFR, and TYMS .
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- HY-157994
-
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EGFR
Apoptosis
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Cancer
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EGFR WT/T790M-IN-2 (Compound 7c) is a EGFR T790M/WT inhibitor with IC50 values of 0.08 and 0.13 μM, respectively. EGFR WT/T790M-IN-2 induces apoptosis by blocking the G0-G1 phase (apoptosis). EGFR WT/T790M-IN-2 has antitumor activity .
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- HY-146442
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Raf
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Cancer
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BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases .
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- HY-115906
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FLT3
MNK
Apoptosis
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Cancer
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K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2 with IC50 values of 680 and 406 nM, respectively. K783-0308 inhibits the growth of MOLM-13 (IC50=10.5 µM) and MV-4-11 (IC50=10.4 µM) cells. K783-0308 promotes acute myeloid leukemia (AML) cell apoptosis and cell cycle arrests in the G0/G1 phase .
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- HY-146887
-
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Deubiquitinase
Apoptosis
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Cancer
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USP7-IN-9 is a highly potent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 value of 40.8 nM. USP7-IN-9 can induce apoptosis and arrest cell progression at G0/G1 and S phases in RS4; 11 cells. USP7-IN-9 reduces the protein levels of oncoproteins MDM2 and DNMT1 and increases the protein levels of tumor suppressors p53 and p21 .
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- HY-150688
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JNK
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Cancer
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JAK3-IN-13 (compound 12n) is a potent, selective and orally active JAK3 inhibitor with IC50 values of 4728, 2039, 8, 365 nM for NK1, JNK2, JNK3, Tyk2, respectively. JAK3-IN-13 shows antiproliferative activity. JAK3-IN-13 induces cell cycle arrest at G0/G1 phase. JAK3-IN-13 shows antitumor activity .
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- HY-162456
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Apoptosis
Reactive Oxygen Species
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Cancer
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Anticancer agent 205 (compound 9) is a potent anticancer agent. Anticancer agent 205 binds to G4-mtDNA target and inhibits the replication, transcription, and translation of mtDNA (mitochondrial genome). Anticancer agent 205 causes mitochondrial dysfunction, increases ROS production, induces DNA damage and cellular senescence. Anticancer agent 205 induces apoptosis and cell cycle arrests at G0/G1 phase. Anticancer agent 205 has the potential for the research of colorectal cancer .
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- HY-149132
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DDA
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LXR
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Cancer
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Dendrogenin A (DDA) is a ligand for liver X receptor (LXR), that induces the expression of sodium/iodine symporter, and increases iodine uptake. Dendrogenin A induces cell differentiation of MCF-7, and reactivates the function of lactating cells. Dendrogenin A induces the expressions of the TSH receptor, thyroid peroxidase, and thyroglobulin, and affects thyroid hormone generation. Dendrogenin A exhibits cytotoxicity in cancer cell B-CPAP and 8505c with IC50 of 4.1 and 6.2 µM. Dendrogenin A arrests the cell cycle at G0/G1 phase .
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- HY-19350
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BML-210
2 Publications Verification
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HDAC
Apoptosis
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Cancer
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BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC50 of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice .
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- HY-131906
-
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JAK
FLT3
Apoptosis
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Cancer
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JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .
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- HY-143246
-
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EGFR
Apoptosis
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Cancer
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EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity .
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- HY-156080
-
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PI3K
Akt
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Cancer
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PI3K-IN-48 is a PI3K inhibitor with IC50 value of 1.55 ± 0.18 μM for A549 cells. PI3K-IN-48 can induce G0/G1 phase arrest, cell apoptosis, and down-regulate expression of p-PI3K and p-Akt. PI3K-IN-48 can be used for human lung cancers diseases research .
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- HY-161966
-
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Apoptosis
Reactive Oxygen Species
VEGFR
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Cancer
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VEGFR-2-IN-52 (compound 14d) is a potent VEGFR-2 inhibitor with an IC50 value of 191.1 nM. VEGFR-2-IN-52 decreases the protein expression of p-VEGFR-2, MMP9, p-ERK1/2 and p-MEK1. VEGFR-2-IN-52 shows cytotoxicity. VEGFR-2-IN-52 induces apoptosis and cell cycle arrest at G0/G1 phase. VEGFR-2-IN-52 increases the levels of ROS .
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- HY-146443
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Raf
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Cancer
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BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases .
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- HY-158138
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PARP
Topoisomerase
Apoptosis
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Cancer
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TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
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- HY-147682
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NF-κB
Apoptosis
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Cancer
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NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
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- HY-152146
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Apoptosis
FGFR
HDAC
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Cancer
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HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity .
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- HY-164384
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PI3K
Akt
mTOR
Apoptosis
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Cancer
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DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
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- HY-147862
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EGFR
Apoptosis
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Cancer
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EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines .
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- HY-146749
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FLT3
Trk Receptor
Apoptosis
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Cancer
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FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML) .
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- HY-130624
-
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HSP
Apoptosis
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Cancer
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Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC50 of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrial membrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549 .
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- HY-159519
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|
Apoptosis
EGFR
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Cancer
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EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
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- HY-161694
-
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DNA Methyltransferase
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Cancer
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DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor .
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- HY-162802
-
|
Apoptosis
PI3K
Akt
PARP
CDK
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Cancer
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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 .
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- HY-126287
-
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Trk Receptor
Apoptosis
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Cancer
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JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
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- HY-123450
-
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Bcr-Abl
Apoptosis
PDGFR
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Cancer
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S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies . S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-152263
-
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PROTACs
CDK
Apoptosis
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Cancer
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HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer . HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-146980
-
|
Apoptosis
GLUT
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Cancer
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GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity .
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- HY-158117
-
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Apoptosis
Autophagy
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Cancer
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[Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 (Compound 3) is a copper complex, which inhibits cell viability of HCT116, HCT116DoxR, A2780 and fibroblasts, with IC50s of 0.13, 0.15, 0.66 and 6.24 μM, respectively. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 induces apoptosis and autophagy, and arrests cell cycle at G0/G1 phase in HCT116DoxR. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 exhibits antimetastatic efficacy .
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-
- HY-124273
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L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0); N-acetyl-L-threo-Sphingosine
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Endogenous Metabolite
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Cardiovascular Disease
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C2 L-threo Ceramide (d18:1/2:0) (L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0)) is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide. C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0/G1 phase and a 7-fold increase in sphingosine accumulation as well as inhibits growth of HL-60 leukemia cells.
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10376
-
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Peptides
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Cancer
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Lucicebtide (Compound ST101) is a selective antagonist for CCAAT/enhancer binding protein β (C/EBPβ). Lucicebtide binds to the leucine zipper domain of C/EBPβ, prevents its dimerization, and ubiquitin-dependently degrades C/EBPβ. Lucicebtide arrests cell cycle at G0/G1 phase. Lucicebtide exhibits cytotoxicity in cancer cells. Lucicebtide exhibits good pharmacokinetic characters and inhibits tumor growth in mouse model .
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- HY-P10376B
-
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Peptides
|
Cancer
|
Lucicebtide acetate is the acetate salt form of Lucicebtide (HY-P10376). Lucicebtide acetate is a selective antagonist for CCAAT/enhancer binding protein β (C/EBPβ). Lucicebtide acetate binds to the leucine zipper domain of C/EBPβ, prevents its dimerization, and ubiquitin-dependently degrades C/EBPβ. Lucicebtide acetate arrests cell cycle at G0/G1 phase. Lucicebtide acetate exhibits cytotoxicity in cancer cells. Lucicebtide acetate exhibits good pharmacokinetic characters and inhibits tumor growth in mouse model .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
|
Classification |
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- HY-159519
-
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Azide
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EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
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