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Aurora kinase-IN-1 (Compound 9) is a potent inhibitor of aurora kinase. Aurora kinase-IN-1 upregulates the expression of G1cellcycle inhibitory proteins including p21 and p27, and G1 progressive cyclin D1, and downregulates G1-to-S progressive cyclins, resulting in cellcycle arrest at the G1/S boundary. Aurora kinase-IN-1 also induces apoptosis. Aurora kinase-IN-1 is a lead compound for chemotherapeutic agents .
Physachenolide C is a potent and selective BET inhibitor that induces apoptosis and arrests the cellcycle in the G0-G1 phase, with antitumor activity .
Typhatifolin B (Compd 2), an anti-cancer agent, could remarkably induce cellapoptosis and G0/G1cycle arrest, as well as block cell migration and invasion .
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1cellcycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
Antiproliferative agent-43 (Compound e4 ) has notable cytotoxic effects against cancer cell lines and causes apoptosis by stopping the cellcycle at G1 phase .
Leptolstatin is an inhibitor of the progression of G1 and G2 phases of the mammalian cellcycle. Leptolstatin can be extracted from the fermentation broth of Streptomyces sp. SAM1595 .
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cellcycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity .
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cellcycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer .
Protosappanin B is a phenolic compound extracted from Caesalpinia sappan. Anti-cancer activity . Protosappanin B induces apoptosis and causes G1cellcycle arrest in human bladder cancer cells .
Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cellcycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
Ganoderic acid DM, a natural triterpenoid isolated from Ganoderma lucidum, induces DNA damage, G1cellcycle arrest and apoptosis in human breast cancer cells. Ganoderic acid DM as a specific inhibitor of osteoclastogenesis .
T2AA is a monoubiquitinated proliferating cell nuclear antigen (PCNA) inhibitor that prevents DNA repair, increases double-strand break (DSB) formation and promotes necroptosis and cellcycle arrest in G1 phase .
p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cellcycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis .
Ganoderic acid Mf is an antitumor triterpenoid. Ganoderic acid Mf causes cellcycle arrest in the G1 phase. Ganoderic acid Mf shows high selectivity between normal and cancer cells and induces cellapoptosis via mitochondria mediated pathway .
Meisoindigo (Dian III), a derivative of Indirubin (HY-N0117), halts the cellcycle at the G0/G1 phase and induces apoptosis in primary acute myeloid leukemia (AML) cells. Meisoindigo exhibits high antitumor activity .
Illudin S, a cytotoxic Illudin, is a natural sesquiterpene with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities. Illudin S blocks the G1-S phase interface of the cellcycle in human leukemia cells .
YM281 is a potent EZH2 inhibitor. YM281 induces cellapoptosis and cellcycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma .
Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1cellcycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cellcycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity .
Antitumor agent-92, an Icaritin (HY-N0678) derivative, causes arrest at the G0/G1 phase in the cellcycle and induces cellapoptosis. Antitumor agent-92 has the potential for hepatocellular carcinoma (HCC) research .
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 cellcycle at G0/G1 phase .
Kazusamycin B is an antibiotic that could be isolated from the fermentation broth of Streptomyces sp. No. 81-484. Kazusamycin B inhibits cell growth and arrests cellcycle at G1 phase. Kazusamycin B can be used in research of cancer .
ZC0109 is a dual inhibitor of IDO1 and thioredoxin reductase 1 (TrxR1) with IC50s of 50 nM and 3.0 μM, respectively. ZC0109 induces ROS accumulation and cellcycle arrest at G1/S phase, thus leads to cancer cellsapoptosis .
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 cellcycle at G0/G1 phase, induces apoptosis in H69AR .
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 cellcycle at G0/G1 phase, and induces apoptosis in Kit mutated cells .
DC-CPin711 is a potent and selective inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 0.0626 μM. DC-CPin711 arrests cellcycle at G1 phase and induces apoptosis .
Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cellcycle at the G0/G1 phase and induces apoptosis .
Antitumor agent-111 (compound 46) is an c-Met kinase inhibitor (IC50=46 nM) with antitumor and antiproliferative activity. Antitumor agent-111 arrests cellcycle at G0/G1 phase, and induces apoptosis .
Antitumor agent-103 (compound 24l) is an apoptosis inducer with antiproliferative and anti-clony formation activities. Antitumor agent-103 arrests cellcycle at G0/G1 phase, enhances NO production, and exhibits anti-tumor activity .
Panduratin A, a natural chalcone compound, is a PPAR-α/δ activator. Panduratin A induces apoptosis, and promotes cellcycle arrest at G0/G1 phase in multiple hematologic malignant cell lines. Panduratin A has anticancer, antioxidant, anti-inflammatory, antibacterial, and antibiofilm activities .
Anticancer agent 204 (Compound 6), a cinnamide fluorinated derivative, possesses anticancer activity. Anticancer agent 204 can arrest the cellcycle of HepG2 cells in the G1 phase and induce apoptosis by reducing the level of mitochondrial membrane polarization (MMP) .
HNHA is a potent histone deacetylase (HDAC) inhibitor. HNHA arrests the cellcycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer .
C2 L-Erythro ceramide (d18:1/2:0) is a cell-permeable sphingolipid. C2 L-Erythro ceramide (d18:1/2:0) induces cellcycle arrest in the G0/G1 phase and inhibits cell growth .
Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1cellcycle arrest, senescence and apoptosis .
Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1cellcycle arrest, senescence and apoptosis .
SK-7041 is a HDAC inhibitor with the IC50 of 172 nM. SK-7041 induces the hyperacetylation of histones H3 and H4 .SK-7041 inhibits tumor cell growth in vivo and in vitro, induces cellapoptosis, and arrests cellcycle at the G1 phase .
Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cellcycle arrest in the G1/S phase of the cellcycle and upregulates p21 WAF1 via a p53 independent manner .
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 cellcycle at both G0-G1 and S phases .
HR488B is an efficient HDAC1 inhibitor. HR488B specifically suppressed the growth of CRC cells by inducing cellcycleG0/G1 arrest and apoptosis. HR488B causes mitochondrial dysfunction, reactive oxygen species (ROS) generation, and DNA damage accumulation .
FLT3-IN-27 (compound 49) is a FLT3-ITD inhibitor with the IC50 of 174 nM. FLT3-IN-27 inhibits cell growth and increases the number of cells in the G1 phase of the cellcycle and can be used for study of acute myeloid leukemia .
MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cellcycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo .
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 cellcycle arrest in G1/G0 phase .
Avadomide is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cellcycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide exhibits potent antitumor and immunomodulatory activities .
cis,trans-Germacrone is a isomer of Germacrone (HY-N0440). Germacrone exhibits a wide range of antitumor, antioxidant and anti-inflammatory effects. Germacrone inhibits lung cancer cell proliferation and alters the Akt/MDM2/p53. Germacrone also arrests cellcycle at G1/S phase .
Apiole (Standard) is the analytical standard of Apiole. This product is intended for research and analytical applications. Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1cellcycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
Suberosin, isolated from Plumbago zeylanica, exhibits anti-inflammatory and anticoagulant activity. Suberosin suppresses PHA-induced PBMC proliferation and arrested cellcycle progression from the G1 transition to the S phase through the modulation of the transcription factors NF-AT and NF-κB .
Maleimide-Val-Ala-PAB-SNS032 is a conjugate of ADC toxin and linker. SNS032 is an inhibitor for CDK, inhibiting the cellcycle at G1/S phase and cell viability of cancer cells. Maleimide-Val-Ala-PAB is a cleavable ADC linker. Maleimide-Val-Ala-PAB-SNS032 can be utilized for the synthesis of ADC molecules .
YS-363 is a potent, selective, and orally active EGFR inhibitor, with IC50s of 0.96 nM and 0.67 nM for wild-type and L858R mutant forms of EGFR, respectively. YS-363 can induce G0/G1cellcycle arrest and apoptosis .
N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cellcycle at G0/G1 phase and induces cellapoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma - .
(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cellcycle 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 .
(+)-Perillyl alcohol is the enantiomer of S-(-)-Perillyl alcohol (HY-116514). (+)-Perillyl alcohol can inhibit the growth of polypeptides and block the cellcycle 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 .
Esterbut-3 is a potent anticancer agent. Esterbut-3 inhibits cell proliferation. Esterbut-3 decreases the antigen expression of 115D8, 140C1 and increases the antigen expression of 123C3. Esterbut-3 induces cellcycle arrest at G0/G1 phase .
Protosappanin B (Standard) is the analytical standard of Protosappanin B. This product is intended for research and analytical applications. Protosappanin B is a phenolic compound extracted from Caesalpinia sappan. Anti-cancer activity . Protosappanin B induces apoptosis and causes G1cellcycle arrest in human bladder cancer cells .
DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cellcycle arrest at sub G1 phase .
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cellcycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cellcycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
VMY-1-103 is an inhibitor for cyclin/Cdk complex, that arrests the cellcycle at G1 phase. VMY-1-103 reduces mitochondrial membrane potential, induces p53 phosphorylation and and PARP cleavage, activates caspase-3, and thus induces apoptosis in prostate cancer cell LNCaP .
Anticancer agent 70 (Compound 21), an anticancer agent, exhibits remarkable cytotoxic activity against numerous human cancer cell lines. Anticancer agent 70 results in the G0/G1-cellcycle arrest with a concomitant increase in p53 and p21 protein levels. Anticancer agent 70 leads to ATP depletion and disruption of the mitochondrial membrane potential .
[1,1′:4′,1′′-Terphenyl]-3,4′′,5-triol (compound 13g) is a terphenyl derivative that blocks the cellcycle 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 .
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 cellapoptosis and arrests the cellcycle at the G0/G1 phase .
Cucurbitacin C is a triterpenoid calabinoid that can be isolated from Cucurbitaceae plants. Cucurbitacin C has anti-cancer activity in vivo and in vitro. Cucurbitacin C can induce cellcycle arrest in G1 or G2/M phase and apoptosis by inhibiting Akt signaling .
GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cellcycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts .
BK50164 is a potent CD73 inhibitor with an IC50 value of 13.089 µM. BK50164 binds to CD99 with a KD value of 1.5 µM. BK50164 shows antiproliferative activity. BK50164 induced Apoptosis and cellcycle arrest at Sub-G1 phase .
BHA536 is an orally active selective inhibitor for PKCα/β and NF-kB signaling pathway. BHA536 inhibits the proliferation of CD79-mutated ABC DLBCL cell, arrests cellcycle at G1 phase, and induces apoptosis in TMD8 cell. BHA536 exhibits antitumor efficacy in mice .
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 cellcycle at G0/G1 phase, and induces apoptosis. rel-Levormeloxifene induces differentation of myelogenesis leukemia, and enhances ROS production in K562 cells .
ALC67 is a cytotoxic thiazolidine compound with an IC50 of approximately 5 μM against liver, breast cancer, colon cancer, and endometrial cancer cell lines. ALC67 induces apoptosis in cancer cells by activating caspase-9 and causing cellcycle arrest at the SubG1/G1 phase, via a pathway that is independent of death receptors. ALC67 can be used in cancer research .
SYHA1815 is an orally active RET inhibitor (IC50=0.9 nmol/L) with antitumor activity. SYHA1815 is more selective for RET than KDR (IC50=15.9 nmol/L). SYHA1815 arrests the G1cellcycle and inhibits RET-driven cell proliferation by downregulating c-Myc .
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 cellcycle in G0/G1 phase. HSP90-IN-23 can be used for cancer research .
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cellcycle 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 .
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 cellcycle arrest at G0/G1 phase. EP26 has the potential for the research of glioblastoma .
EGFR-IN-131 (compound 3a) is a potent and cross the blood-brain barrier EGFR inhibitor with an IC50 value of 272.9 nM. EGFR-IN-131 shows antiproliferative activity. EGFR-IN-131 induces apoptosis and cellcycle arrest at G0/G1 phase. EGFR-IN-131 decreases the protein expression of p-EGFR .
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 cellcycle at phase G0/G1 .
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 cellcycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs) .
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 cellcycle arrest and apoptosis in MDA-MB-231 breast cancer cells, and it inhibits the proliferation and invasion of breast cancer cell lines .
Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cellcycle arrest at sub-G1 phase .
Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin arrests cellcycle at G1 and G2/M phase. Lobaplatin induces apoptosis by increasing expressions of caspase and Bax, decreasing expression of Bcl-2. Lobaplatin can be used for research of cancer .
Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and abrogates cellcycle progression at G1 and S phases. Hygrolidin has antitumor activity .
VEGFR-2-IN-23 (compound 11b) is a potent and selective VEGFR-2 inhibitor with an IC50 value of 0.34 nM. VEGFR-2-IN-23 shows antitumor activity. VEGFR-2-IN-23 induces apoptosis and cellcycle arrest at G1 phase .
INX-315 is an orally active and selective CDK2 inhibitor that induces cellcycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
Secalonic acid D is a toxic compound against tumor cells. Secalonic acid D can be isolated from the metabolites of Aspergillus aculeatus. Secalonic acid D activates GSK3-β, and degrades β-catenin. Thus, Secalonic acid D down-regulates c-Myc expression, arrests cellcycle at G1 phase, induces cellapoptosis .
Cantharidic acid is a selective inhibitor for protein phosphatase 2 (PP2A) and protein phosphatase 1 (PP1). Cantharidic acid inhibits cell viability and arrest cellcycle at sub G1 phase, induces apoptosis in cells NPC-39 and HONE-1 through the upregulation of ERK1/2, p38, and JNK1/2 pathway .
Avadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active cereblon modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cellcycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities .
Milademetan tosylate is the tosylate salt form of Milademetan (HY-101266). Milademetan tosylate is an orally active inhibitor for MDM2. Milademetan tosylate arrests the cellcycle at G1 pahse, induces the apoptosis Milademetan tosylate restores the p53 activity by targeting the p53-MDM2 interaction, and exhibits anticancer activity against Merkel cell carcinoma (MCC) .
Antiproliferative agent-63 (compound 4d), a ring-annulated analogue of Cannabidiol, is an anticancer agent. Antiproliferative agent-63 demonstrates a promising activity against breast and colorectal cancer. Antiproliferative agent-63 arrests the G1 phase of the cellcycle and induces apoptosis via the mitochondrial pathway in breast cancer cell lines .
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 cellcycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .
FB49 is a highly selective inhibitor of Bcl-2-associated athanogene 3 (BAG3), with the Ki of 45 μM. FB49 inhibits the cell growth in human tumoral cells, but has no toxicity in human peripheral mononuclear cells. FB49 block cellcycle in G1 phase and to induce apoptosis as well as autophagy in medulloblastoma HD-MB03 treated cells .
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 cellcycle 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 .
DH-18 is a matrix metalloproteinase-2 (MMP-2) inhibitor with the IC50 values of 139.45 nM, 518.11 nM and 833.34 nM for MMP-2, MMP-9 and MMP-8, respectively. DH-18 induces cellapoptosis and arrests cellcycle in the G0/G1 phase. DH-18 inhibits cell growth and can be used for study of chronic myeloid leukemia .
FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cellcycle arrest at pre-G1 and G2/M phase .
Antiproliferative agent-26 (compound 4g) is an antiproliferative agent with much broad range of activity targeting Leukemia, CNS, Melanoma, Renal and Breast (at the concentration of 10 μM). Antiproliferative agent-26 inhibits colony forming and arrests cellcycle at G1 phase/S phase at 5 μM and 25 μM, respectively .
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1cellcycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857) .
SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1cellcycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857) .
RET/TRKA-IN-1 (Compound 13) is a dual inhibitor for RET (IC50=0.375 µM) and TRKA. RET/TRKA-IN-1 inhibits cell viability of LC-2 and KM12, with GI50 of 0.72 and 0.25 μM. RET/TRKA-IN-1 arrests the cellcycle at G1 phase .
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cellcycle at G0/G1 .
AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC50 value of 0.55 μM. AKT-IN-12 induces G0/G1cellcycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia .
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 cellcycle into the G0/G1 phase .
ALK/EGFR-IN-2 is a potent dual inhibitor of ALK and EGFR. ALK/EGFR-IN-2 induces apoptosis and G0/G1cellcycle arrest in cancer cells. ALK/EGFR-IN-2 significantly inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively .
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 cellcycle arrest in G0/G1 phase and induces tumor cellapoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies .
Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cellcycle 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 .
14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a KD of 35 µM. 14-3-3η Protein inhibitor 1 shows inhibitory activities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cellapoptosis and G1-S cellcycle arrest with good metabolic stability .
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cellcycle at the G1 phase and induce MCF-7 cellsapoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin .
Cu(II)-Elesclomol is a Cu 2+ complex of Elesclomol (HY-12040). Cu(II)-Elesclomol induces cuproptosis. Cu(II)-Elesclomol also inducesapoptosis, causes a G1cellcycle block and induces DNA double strand breaks in K562 cells. Cu(II)-Elesclomol also weakly inhibits DNA topoisomerase I. Cu(II)-Elesclomol has anticancer activity .
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cellcycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
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 cellcycle arrest at G0/G1 phase. Menin-MLL inhibitor-25 reverses the differentiation arrest .
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 cellcycle at G0/G1 phase .
Apoptosis inducer 30 (Compound 15a) is an anticancer agent. Apoptosis inducer 30 induces MCF-7 cellsapoptosis through mitochondrial pathway. Apoptosis inducer 30 induces intracellular reactive oxygen species levels and decreases mitochondrial membrane potential, and blocks the cellcycle in the G0/G1 phase. Apoptosis inducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and inhibits tumor growth in a mouse model of breast cancer .
PI3K/mTOR Inhibitor-8 (Compound 18b) is a PI3K and mTOR dual inhibitor with IC50 values of 0.46 nM and 12 nM against PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-8 induces HCT-116 cellsapoptosis and arrests cellcycle at the G1/S phase .
GP130-IN-1 (compound 49) is a potent GP130 inhibitor with significant in vitro antitumor activity and higher selectivity than Bazedoxifene (HY-A0031). GP130-IN-1 induces ultrastructural changes in cells, causing cellcycle arrest in the G0/G1 phase in a time-dependent manner and triggering apoptosis and autophagy. GP130-IN-1 can be used in the study of triple-negative breast cancer .
Angelylalkannin is a naphthoquinone compound isolated from the root of Alkanna tinctoria. Angelylalkannin showed significant inhibitory effects in the antiproliferative effect test on human colon cancer cells HCT-116 and SW-480. The median inhibitory concentration (IC50) of Angelylalkannin was 4.76 mM for HCT-116 cells and 7.03 mM for SW-480 cells. Like alkannin, Angelylalkannin can arrest the cellcycle in the G1 phase and induce apoptosis at a concentration of 1-10 mM.
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 .
VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cellcycle mainly in the G1/S phase .
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 cellcycle 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 .
Antitumor agent-182 (Compound 12a) decreases mitochondrial membrane potential (MMP) and enhances ROS levels. Antitumor agent-182 arrests the cellcycle 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 .
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 cellcycle arrest at G0/G1 phase. HDAC6-IN-48 increases the protein expression of acetylated α-tubulin .
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 cellcycle arrest at G0/G1 phase. HS-438 shows antitumor activity. HS-438 has the potential for the research of chronic myeloid leukemia (CML) .
HSP90-IN-33 (compound 24e) is a potent Hsp90 inhibitor with Kd values of ≥200, 7.3 µM for Hsp90α, Hsp90β, respectively. HSP90-IN-33 induces apoptosis and cellcycle arrest at G0/G1 phase. HSP90-IN-33 decreases the protein expression of ERα, CDK4 and Akt .
Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cellcycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
Antitumor agent-159 (Compound 13b) targets the mitochondria and downregulates cardiolipin levels. Antitumor agent-159 inhibits the proliferation of cancer cell MDA-MB-231, arrests the cellcycle at sub-G1 phase, and induces apoptosis in MDA-MB-231. Antitumor agent-159 exhibits antitumor efficacy in MDA-MB-231 xenograft mouse models .
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) cellapoptosis and cellcycle arrests in the G0/G1 phase .
Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cellcycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity .Tunicamycin increases exosome release in cervical cancer cells .
YCH3124 (compound Z33) is a USP7 inhibitor (IC50=41.9 nM) with antitumor activity. YCH3124 has good in vitro antiproliferative activity against various tumor cells including LNCaP (IC50=3.6 nM) and CHP-212 (IC50=9.9 nM). In addition, YCH3124 disrupts cellcycle progression by restricting G1 phase and induces apoptosis in CHP-212 cells .
Amentoflavone (Standard) is the analytical standard of Amentoflavone. This product is intended for research and analytical applications. Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cellcycle arrest at sub-G1 phase .
BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cellcycle 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 .
HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC50 values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cellapoptosis, G0/G1cellcycle arrest, and blocks migration and invasion .
7-Hydroxystaurosporine (UCN-01) is a synthetic derivative of Staurosporine (HY-15141) with antitumor activity. 7-hydroxystaurosporine inhibits serine/threonine kinase AKT and calcium-dependent protein kinase C activity. 7-hydroxystaurosporine also activates indirectly cyclin-dependent kinases (CDKs). 7-hydroxystaurosporine arrests tumor cells in the G1/S of the cellcycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis .
EGFR-IN-137 (Compound 4c) is an inhibitor for aromatase and EGFR with IC50s of 1.67 μg/mL and 0.08 μg/mL. EGFR-IN-137 inhibits the proliferation of cancer cell MCF-7 and MDA-MB-231 with IC50s of 1.62 µM and 4.14 µM. EGFR-IN-137 arrests the cellcycle at G0/G1 phase in MDA-MB-231, and induces apoptosis through caspase-dependent pathway .
EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cellcycle at G1/S and induces cellsapoptosis .
Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cellcycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
HX531 is an effective RXR antagonist with oral activity, with an IC50 of 18 nM, with activity against black melanoma. HC531 can eliminate the anti-apoptotic effects of all-trans-retinoic acid (t-RA) and exerts anti-obesity and anti-diabetic effects through leptin-dependent pathways and the p53-p21Cip1 pathway, resulting in G0/G1cellcycle arrest .
BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1cycle-arresting activity .
L 741742 is a dopamine receptor D4 (DRD4) antagonist that selectively inhibits glioblastomas (GBM) growth in vitro and in vivo, synergyed with Temozolomide (TMZ) (HY-17364). L 741742 disrupts in effectors PDGFRβ/ERK1/2 and mTOR signaling. Additionally, L 741742 disrupts endolysosmal function compromising the autophagy-lysosomal degradation pathway, followed by G0/G1cellcycle arrest and Apoptosis. L 741742 is promising for research of GBM and neurogenesis .
SILA-123 is a FLT3 inhibitor (FLT3-WT: IC50=2.1 nM; FLT3-ITD: IC50=1.0 nM). SILA-123 inhibits FLT3 phosphorylation and downstream signaling pathways, leading to apoptosis by arresting cellcycle progression at the G0/G1 phase. SILA-123 can be used in the study of acute myeloid leukemia .
Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cellcycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities .
CDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cellcycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .
CTL-06 is an inhibitor of Fatty Acid Synthase (FASN) (IC50: 3 μM) and can induce apoptosis. CTL-12 blocks the cellcycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
CDK4/6-IN-15 hydrochloride is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 hydrochloride potently inhibits cancer cells growth. CDK4/6-IN-15 hydrochloride arrests cellcycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .
Apoptosis Inducer 28 (Compound X1) is an apoptosis-inducing agent with anticancer activity in vitro. Apoptosis Inducer 28 can arrest the cellcycle at the G1 phase, promote cell death, and induce apoptosis by disrupting mitochondrial membrane potential. Apoptosis inducer 28 can also decrease the production of reactive oxygen species, downregulate the gene expression of BAX, Bcl-xL, and Bcl-2, while upregulating the gene expression of PAR-4 .
ZDLD20, a β-carboline, is orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 6.51 μM. ZDLD20 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cellcycle. ZDLD20 exhibits potent anticancer activity .
VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cellcycle mainly in the G1 phase .
FLT3-IN-18 is a potent and selective FLT3 inhibitor with an IC50 value of 0.003 μM. FLT3-IN-18 induces apoptosis and cellcycle arrest at G1 phase. FLT3-IN-18 inhibits FLT3 and STAT5 phosphorylation. FLT3-IN-18 has the potential for the research of acute myeloid leukemia (AML) .
AKT-IN-25 (Compound 14a) is an inhibitor for Akt, that inhibits the phosphorylation of Akt, and thereby inhibits the PI3K/Akt/mTOR signaling pathway. AKT-IN-25 arrests the cellcycle at G1 phase, inhibits the cell migration of PANC-1, and inhibits the proliferation of cancer cells PANC-1, PATU-T, and SUIT-2 with IC50s of 3.05, 1.32, and 3.85 μM, respectively .
JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617Fcells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cellcycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cellcycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases .
N6-Benzyladenosine-d5 (Benzyladenosine-d5) is deuterium labeled N6-Benzyladenosine. N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cellcycle at G0/G1 phase and induces cellapoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma .
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 cellcycle arrests at G0/G1 phase. Anticancer agent 205 has the potential for the research of colorectal cancer .
CTL-12 is an inhibitor of fatty acid synthase (FASN) (IC50: 2.5 μM) and can induce apoptosis. CTL-12 blocks the cellcycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cellcycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model .
JUN-1111 is an irreversible and selective Cdc25 phosphatase inhibitor with IC50 values of 0.38, 1.8, 0.66, 28, 37 µM for Cdc25A, Cdc25B, Cdc25C, VHR, PTP1B, respectively. JUN-1111 induces cellcycle arrest at G1 and G2/M phases. JUN-1111 decreases the expression of phosphoCdk1 .
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 cellcycle 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 .
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 cellcycle 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% .
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 cellcycle arrest in G0/G1 phase .
BML-278 is a SIRT1 activator (EC150: 1 μM). BML-278 increases H3K9 methylation and inhibits H3K9 acetylation in both the paternal and maternal pronucleus. BML-278 improves early embryonic development. BML-278 arrests the cellcycle at the G1/S phase, and reduces senescence in primary human mesenchymal cells. BML-278 reduces tubulin acetylation in U937 cells. BML-278 also increases mitochondrial density in murine C2C12 myoblasts .
RK-682 is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cellcycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24 .
Atractylenolide II (Standard) is the analytical standard of Atractylenolide II. This product is intended for research and analytical applications. Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cellcycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
Decursin (Standard) is the analytical standard of Decursin. This product is intended for research and analytical applications. Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cellcycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities [4].
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cellcycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
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 cellcycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor .
Carvacrol (Standard) is the analytical standard of Carvacrol. This product is intended for research and analytical applications. Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cellcycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
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 cellcycle arrest at G0/G1 phase. VEGFR-2-IN-52 increases the levels of ROS .
EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cellcycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cellapoptosis .
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cellcycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .
PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM. PROTAC CDK4/6 degrader 1 inhibits the proliferation of cell Jurkat (IC50 is 0.18 μM), arrests the cellcycle at G1 phase and induces apoptosis. (Pink: ligand for target protein YY173 (HY-163787); Black: linker (HY-163788); Blue: ligand for E3 ligase (HY-10984))
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 cellcycle at G0/G1 phase in A549 .
PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cellcycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.) .
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 cellcycle 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 .
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 cellcycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity .
1-Octanol-d5 is deuterated labeled Carvacrol (HY-N0711). Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cellcycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
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 cellcycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cellcycle. FD223 has potential for the research of leukemia such as AML .
WJ35435 is a dual-targeted anticancer hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and anti-topoisomerase I activities that causes DNA damage associated with a low DNA repair capability and induces cellcycle arrest at G1- and G2-phase to apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect. WJ35435 is promising for research of cancer .
EGFR-IN-134 (compound 3f), a triazolo[3,4-a]isoquinoline derivative, is a potent EGFR inhibitor with an IC50 of 0.023 µM. EGFR-IN-134 induces apoptosis and necrosis. EGFR-IN-134 initiates cellcycle arrest at the G2/M and pre-G1 phases, downregulates anti-apoptotic protein Bcl2 and upregulates pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. EGFR-IN-134 shows antiproliferative and anticancer activity .
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 cellcycle 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) .
Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cellcycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease .
PROTAC c-Met degrader-1 (Compound Met-DD4) is an orally active PROTAC degrader for c-Met with a DC50 of 6.21 nM. PROTAC c-Met degrader-1 inhibits the proliferation of c-Met-addicted cell MKN-45 with an IC50 of 4.37 nM, and arrests the cellcycle at G0/G1 phase. PROTAC c-Met degrader-1 exhibits antitumor efficacy in MKN-45 xenograft mouse models . (Pink: Ligand for target protein (HY-13404); Blue: Ligand for E3 ligase (HY-W087383); Black: Linker (HY-W074901))
SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2 with an IC50 of 1.2 μM. In cellular studies, SHP2-IN-33 demonstrates antiproliferative activity with an IC50 of 38 μM against Huh7 cells by arresting the G0/G1cellcycle, promoting apoptosis (Apoptosis), and suppressing the MAPK signaling pathway. In an in vivo Huh7 xenograft mouse model, SHP2-IN-33 exhibits significant antitumor activity and favorable pharmacokinetics, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 is a promising compound for studying tumor diseases associated with SHP2 .
RK-682 hemicalcium is the hemicalcium salt form of RK-682 (HY-135564A). RK-682 hemicalcium is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 hemicalcium inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 hemicalcium inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cellcycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24 [2] .
HDAC-IN-56 ((S)-17b) is an orally active class I histone deacetylase (HDAC) inhibitor with IC50 values of 56.0 ± 6.0, 90.0 ± 5.9, 422.2 ± 105.1, >10000 nM for HDAC1, HDAC2, HDAC3, and HDAC4-11, respectively. HDAC-IN-56 has potent inhibitory activity while strongly increasing intracellular levels of acetylhistone H3 and P21 and effectively inducing G1cellcycle arrest and apoptosis.HDAC-IN-56 has antitumor activity .
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 cellcycle, 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.
PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC50 of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cellcycle arrest at G2/M phase .
PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cellcycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy .
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 cellcycle 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.
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 cellcycle, 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 .
PROTAC EZH2 Degrader-3 (compound ZJ-20) is a EZH2 PROTAC degrader. PROTAC EZH2 Degrader-3 (5 μM, 24 h) not only potently inhibits the expression of EZH2 protein, but also had a strong inhibits effect on the expression levels of other subunits of PRC2 as well as H3k27me3 protein. PROTAC EZH2 Degrader-3 shows anti-proliferative activity and blocks the cellcycle in the G0-G1 phase and induces cellapoptosis((Blue: cereblon ligand Pomalidomide (HY-10984), Black: linker HY-W361751；Pink: EZH2 inhibitor Tazemetostat (HY-13803)) .
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cellcycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cellcycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrial membrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models .
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 cellcycle arrest in the G0/G1 phase and a 7-fold increase in sphingosine accumulation as well as inhibits growth of HL-60 leukemia cells.
SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cellcycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM) .
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cellcycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively .
[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 cellcycle at G0/G1 phase in HCT116DoxR. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 exhibits antimetastatic efficacy .
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cellcycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2.
PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM.
PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .
EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cellcycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity .
CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively .
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 cellapoptosis and cellcycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity .
Ethylenediaminediacetic acid (N,N-Ethylenediglycine) is an important ligand that enhances the antiproliferative activity of metal complexes. The complexes formed by ethylenediacetic acid and metal ions exhibited significant antiproliferative properties in MCF-7 cancer cell line. The metal complexes of ethylenediacetic acid were able to interact with DNA and were studied by CD and EPR spectroscopy techniques. Ethylenediaminediacetic acid and its metal complexes were able to induce cellcycle arrest at the G(0)/G(1) phase. The crystal structure analysis of ethylenediacetic acid provided important structural information for understanding its biological activity .
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cellcycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer .
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1cellcycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
TAT-p16 (p16INK4a peptide) is a peptide mimic of p16INK4a that can induce an early G phase cellcycle arrest in the absence of active cyclin E:Cdk2 complex .
Protosappanin B is a phenolic compound extracted from Caesalpinia sappan. Anti-cancer activity . Protosappanin B induces apoptosis and causes G1cellcycle arrest in human bladder cancer cells .
Ganoderic acid DM, a natural triterpenoid isolated from Ganoderma lucidum, induces DNA damage, G1cellcycle arrest and apoptosis in human breast cancer cells. Ganoderic acid DM as a specific inhibitor of osteoclastogenesis .
Meisoindigo (Dian III), a derivative of Indirubin (HY-N0117), halts the cellcycle at the G0/G1 phase and induces apoptosis in primary acute myeloid leukemia (AML) cells. Meisoindigo exhibits high antitumor activity .
Illudin S, a cytotoxic Illudin, is a natural sesquiterpene with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities. Illudin S blocks the G1-S phase interface of the cellcycle in human leukemia cells .
Physachenolide C is a potent and selective BET inhibitor that induces apoptosis and arrests the cellcycle in the G0-G1 phase, with antitumor activity .
Typhatifolin B (Compd 2), an anti-cancer agent, could remarkably induce cellapoptosis and G0/G1cycle arrest, as well as block cell migration and invasion .
Leptolstatin is an inhibitor of the progression of G1 and G2 phases of the mammalian cellcycle. Leptolstatin can be extracted from the fermentation broth of Streptomyces sp. SAM1595 .
Ganoderic acid Mf is an antitumor triterpenoid. Ganoderic acid Mf causes cellcycle arrest in the G1 phase. Ganoderic acid Mf shows high selectivity between normal and cancer cells and induces cellapoptosis via mitochondria mediated pathway .
Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1cellcycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
Panduratin A, a natural chalcone compound, is a PPAR-α/δ activator. Panduratin A induces apoptosis, and promotes cellcycle arrest at G0/G1 phase in multiple hematologic malignant cell lines. Panduratin A has anticancer, antioxidant, anti-inflammatory, antibacterial, and antibiofilm activities .
Apiole (Standard) is the analytical standard of Apiole. This product is intended for research and analytical applications. Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1cellcycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
Suberosin, isolated from Plumbago zeylanica, exhibits anti-inflammatory and anticoagulant activity. Suberosin suppresses PHA-induced PBMC proliferation and arrested cellcycle progression from the G1 transition to the S phase through the modulation of the transcription factors NF-AT and NF-κB .
N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cellcycle at G0/G1 phase and induces cellapoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma - .
(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cellcycle 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 .
Protosappanin B (Standard) is the analytical standard of Protosappanin B. This product is intended for research and analytical applications. Protosappanin B is a phenolic compound extracted from Caesalpinia sappan. Anti-cancer activity . Protosappanin B induces apoptosis and causes G1cellcycle arrest in human bladder cancer cells .
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cellcycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
Cucurbitacin C is a triterpenoid calabinoid that can be isolated from Cucurbitaceae plants. Cucurbitacin C has anti-cancer activity in vivo and in vitro. Cucurbitacin C can induce cellcycle arrest in G1 or G2/M phase and apoptosis by inhibiting Akt signaling .
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cellcycle 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 .
Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cellcycle arrest at sub-G1 phase .
Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and abrogates cellcycle progression at G1 and S phases. Hygrolidin has antitumor activity .
Secalonic acid D is a toxic compound against tumor cells. Secalonic acid D can be isolated from the metabolites of Aspergillus aculeatus. Secalonic acid D activates GSK3-β, and degrades β-catenin. Thus, Secalonic acid D down-regulates c-Myc expression, arrests cellcycle at G1 phase, induces cellapoptosis .
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 cellcycle 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 .
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cellcycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
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 cellcycle at G0/G1 phase .
Angelylalkannin is a naphthoquinone compound isolated from the root of Alkanna tinctoria. Angelylalkannin showed significant inhibitory effects in the antiproliferative effect test on human colon cancer cells HCT-116 and SW-480. The median inhibitory concentration (IC50) of Angelylalkannin was 4.76 mM for HCT-116 cells and 7.03 mM for SW-480 cells. Like alkannin, Angelylalkannin can arrest the cellcycle in the G1 phase and induce apoptosis at a concentration of 1-10 mM.
Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cellcycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cellcycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity .Tunicamycin increases exosome release in cervical cancer cells .
Amentoflavone (Standard) is the analytical standard of Amentoflavone. This product is intended for research and analytical applications. Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cellcycle arrest at sub-G1 phase .
Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cellcycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cellcycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities .
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cellcycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases .
Atractylenolide II (Standard) is the analytical standard of Atractylenolide II. This product is intended for research and analytical applications. Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cellcycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
Decursin (Standard) is the analytical standard of Decursin. This product is intended for research and analytical applications. Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cellcycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities [4].
Carvacrol (Standard) is the analytical standard of Carvacrol. This product is intended for research and analytical applications. Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cellcycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
CDK1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cellcycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; DKFZp686L20222
The CDK1/CDC2-cyclin-B complex is a key regulator in the cell cycle. It plays an important role in cell division and development and regulates a variety of cellular activities, including chromosome segregation, nuclear membrane rupture, cytokinesis, etc. The activity of CDK1 is regulated by a variety of phosphorylation and dephosphorylation, thereby controlling the progression of the cell cycle and the DNA repair process. CDK1-CCNA2 Protein, Human (sf9, GST, His) is the recombinant human-derived CDK1-CCNA2, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. ,
CDK1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cellcycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; DKFZp686L20222
The CDK1/CDC2-cyclin-B complex is a key regulator in the cell cycle. It plays an important role in cell division and development and regulates a variety of cellular activities, including chromosome segregation, nuclear membrane rupture, cytokinesis, etc. The activity of CDK1 is regulated by a variety of phosphorylation and dephosphorylation, thereby controlling the progression of the cell cycle and the DNA repair process. CDK1-CCNE1 Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK1-CCNE1, expressed by Sf9 insect cells , with N-GST, N-Flag, N-His labeled tag. ,
CDK1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cellcycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; DKFZp686L20222
The CDK1/CDC2-cyclin-B complex is a key regulator in the cell cycle. It plays an important role in cell division and development and regulates a variety of cellular activities, including chromosome segregation, nuclear membrane rupture, cytokinesis, etc. The activity of CDK1 is regulated by a variety of phosphorylation and dephosphorylation, thereby controlling the progression of the cell cycle and the DNA repair process. CDK1-CCNE2 Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK1-CCNE2, expressed by Sf9 insect cells , with N-His, N-GST, N-Flag labeled tag. ,
CDK1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cellcycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; DKFZp686L20222
N6-Benzyladenosine-d5 (Benzyladenosine-d5) is deuterium labeled N6-Benzyladenosine. N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cellcycle at G0/G1 phase and induces cellapoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma .
1-Octanol-d5 is deuterated labeled Carvacrol (HY-N0711). Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cellcycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
TAT-p16 (p16INK4a peptide) is a peptide mimic of p16INK4a that can induce an early G phase cellcycle arrest in the absence of active cyclin E:Cdk2 complex .
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 cellcycle 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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