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G1 and S-phases

" in MedChemExpress (MCE) Product Catalog:

42

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1

Peptides

3

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-113638
    CVT-11127

    GS-456332

    		 Stearoyl-CoA Desaturase (SCD) Apoptosis Cancer
    CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer .
    CVT-11127
  • HY-125098
    Illudin S
    1 Publications Verification

    		 DNA Alkylator/Crosslinker Apoptosis Infection Cancer
    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 cell cycle in human leukemia cells .
    Illudin S
  • HY-118672
    HNHA

    		HDAC MMP HIF/HIF Prolyl-Hydroxylase Cancer
    HNHA is a potent HDAC inhibitor with an IC50 of 100 nM. HNHA arrests the cell cycle 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 .
    HNHA
  • HY-151978
    ZC0109

    		Indoleamine 2,3-Dioxygenase (IDO) Apoptosis 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 cell cycle arrest at G1/S phase, thus leads to cancer cells apoptosis .
    ZC0109
  • HY-N1196
    Suberosin

    		NF-κB Inflammation/Immunology
    Suberosin, isolated from Plumbago zeylanica, exhibits anti-inflammatory and anticoagulant activity. Suberosin suppresses PHA-induced PBMC proliferation and arrested cell cycle progression from the G1 transition to the S phase through the modulation of the transcription factors NF-AT and NF-κB .
    Suberosin
  • HY-155552
    GSPT1 degrader-1

    		Molecular Glues Apoptosis Cancer
    GSPT1 degrader-1 (compound 9q) is a potent degrader of G1 to S phase transition 1 (GSPT1) via ubiquitin-proteasome system, serves as one of Molecular Glues. GSPT1 degrader-1 also induces cell G0/G1 phase arrest and apoptosis .
    GSPT1 degrader-1
  • HY-152135
    TJ08

    		Apoptosis Cancer
    TJ08, a 1,2,5-trisubstituted benzimidazole derivative, efficiently induces G1/S phase arrest and promotes apoptosis in various cancer cells. TJ08 is an anticancer agent .
    TJ08
  • HY-13768C
    Topotecan hydrochloride hydrate

    SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate

    		 Topoisomerase Apoptosis Autophagy Cancer
    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 .
    Topotecan hydrochloride hydrate
  • HY-13768
    Topotecan

    SKF 104864A; NSC 609669

    		 Topoisomerase Autophagy Apoptosis Cancer
    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 .
    Topotecan
  • HY-163722
    EGFR/DHFR-IN-1

    		EGFR Dihydrofolate reductase (DHFR) Cancer
    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 .
    EGFR/DHFR-IN-1
  • HY-145670
    cis,trans-Germacrone

    		Akt MDM-2/p53 Cancer
    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 cell cycle at G1/S phase .
    cis,trans-Germacrone
  • HY-145963
    DRB18

    		GLUT Cancer
    DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity .
    DRB18
  • HY-133537
    Hygrolidin

    		Antibiotic Fungal ADC Payload Infection 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 cell cycle progression at G1 and S phases. Hygrolidin has antitumor activity .
    Hygrolidin
  • HY-161780
    Maleimide-PEG8-Val-Ala-PAB-SNS032

    		Drug-Linker Conjugates for ADC CDK Cancer
    Maleimide-Val-Ala-PAB-SNS032 is a conjugate of ADC toxin and linker. SNS032 is an inhibitor for CDK, inhibiting the cell cycle 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 .
    Maleimide-PEG8-Val-Ala-PAB-SNS032
  • HY-156470
    Multi-kinase-IN-6

    		Trk Receptor Anaplastic lymphoma kinase (ALK) c-Kit EGFR Pim Casein Kinase Checkpoint Kinase (Chk) CDK Apoptosis Cancer
    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 cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
    Multi-kinase-IN-6
  • HY-155055
    Antiproliferative agent-26

    		Others Cancer
    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 cell cycle at G1 phase/S phase at 5 μM and 25 μM, respectively .
    Antiproliferative agent-26
  • HY-146038
    Antitumor agent-55

    		Apoptosis ROS Kinase MDM-2/p53 Bcl-2 Family Cancer
    Antitumor agent-55 (compound 5q) is a potent antitumor agent. Antitumor agent-55 effectively inhibits PC3, with an IC50 of 0.91 μM. Antitumor agent-55 effectively inhibits the colony formation, suppresses the cell migration in PC3. Antitumor agent-55 induces G1/S phase arrest and apoptosis in PC3 .
    Antitumor agent-55
  • HY-13721
    Phenoxodiol
    3 Publications Verification

    Idronoxil; Dehydroequol; Haginin E

    		 Caspase Apoptosis Topoisomerase Cancer
    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 cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner .
    Phenoxodiol
  • HY-146491
    VEGFR-2/BRAF-IN-1

    		VEGFR Raf Apoptosis Cancer
    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 cell cycle mainly in the G1/S phase .
    VEGFR-2/BRAF-IN-1
  • HY-151630
    hCAIX-IN-16

    		Carbonic Anhydrase Cancer
    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 .
    hCAIX-IN-16
  • HY-13721R
    Phenoxodiol (Standard)

    		Caspase Apoptosis Topoisomerase Cancer
    Phenoxodiol (Standard) is the analytical standard of Phenoxodiol. This product is intended for research and analytical applications. 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 cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner .
    Phenoxodiol (Standard)
  • HY-172111
    EGFR-IN-144

    		EGFR Microtubule/Tubulin Interleukin Related TNF Receptor Apoptosis Cancer
    EGFR-IN-144 (Compound 4B) exhibits inhibitory activities against EGFR (IC50=0.639 µg/mL) and tubulin polymerization (IC50=7.339 µg/mL). EGFR-IN-144 exhibits cytotoxicity in multiple cancer cell with GI50 of nanomolare levels. EGFR-IN-144 downregulates the expressions of mTOR, TNF-α, and IL-6, arrests the cell cycle at G1/S phase, and induces apoptosis .
    EGFR-IN-144
  • HY-146200
    PI3K/mTOR Inhibitor-8

    		PI3K mTOR 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 cells apoptosis and arrests cell cycle at the G1/S phase .
    PI3K/mTOR Inhibitor-8
  • HY-172897
    EGFR/DHFR-IN-2

    		EGFR Dihydrofolate reductase (DHFR) Apoptosis Cytochrome P450 Cancer
    EGFR/DHFR-IN-2 (9b) is a dual h-DHFR/EGFR TK inhibitor, with IC50 values of 0.192 μM and 0.109 μM for h-DHFR and EGFR, respectively. EGFR/DHFR-IN-2 (9b) halts the cell cycle at the G1/S phase and induces apoptosis. EGFR/DHFR-IN-2 (9b) is a potential inhibitor of CYP2C9 and CYP3A4. EGFR/DHFR-IN-2 (9b) can be used in the cancer research .
    EGFR/DHFR-IN-2
  • HY-146887
    USP7-IN-9

    		Deubiquitinase Apoptosis Cancer
    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 .
    USP7-IN-9
  • HY-158106
    AZD8421

    		CDK Cancer
    AZD8421 is a selective CDK2 inhibitor (IC50 = 9 nM) as well as achieving CDK family selectivity in cells versus key off-targets (CDK1, CDK4/6, CDK9), AZD8421 had no significant kinase inhibition outside the CDK family. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest in G1/S phase and senescence. AZD8421 can be studied in research for breast cancer and ovarian cancer .
    AZD8421
  • HY-149540
    CTL-06

    		Fatty Acid Synthase (FASN) Cancer
    CTL-06 is an inhibitor of Fatty Acid Synthase (FASN) (IC50: 3 μM) and can induce apoptosis. CTL-12 blocks the cell cycle 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 .
    CTL-06
  • HY-146750
    HDAC-IN-37

    		HDAC Apoptosis Cancer
    HDAC-IN-37 is a potent HDAC inhibitor with IC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM for HDAC1, HDAC3, HDAC8 and HDAC6, respectively. HDAC-IN-37 induces histone acetylation in a slow-off manner. HDAC-IN-37 prevents cell transition from G1 phase to S phase and induces early cell apoptosis .
    HDAC-IN-37
  • HY-172092
    BG11

    		Apoptosis Ferroptosis Cancer
    BG11 induces the accumulation of Fe 2+ and intracellular lipid peroxides, induces ferroptosis. BG11 regulates the expression of Bax and Bcl-2 proteins, and induces apoptosis in MDA-MB-231 cell. BG11 arrests the cell cycle at G0/G1 and S phase, inhibits the proliferation of TNBC cancer cell (IC50 for MDA-MB-231 and BT549 is 0.49 μM and 0.52 μM), and inhibits the cell migration and invasion. BG11 exhibits antitumor efficacy in mouse models .
    BG11
  • HY-149541
    CTL-12

    		Fatty Acid Synthase (FASN) Cancer
    CTL-12 is an inhibitor of fatty acid synthase (FASN) (IC50: 2.5 μM) and can induce apoptosis. CTL-12 blocks the cell cycle 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 .
    CTL-12
  • HY-170992
    Autophagy agonist-1

    		Autophagy CDK Atg8/LC3 PINK1/Parkin Cancer
    Autophagy agonist-1 (compound 22) is an Autophagy agonist. Autophagy agonist-1 exhibits significant anticancer activity against HepG2 cells and normal cells with IC50s of 8.8 μM and > 50 μM. Autophagy agonist-1 induces G1/S phase cell cycle arrest and inhibits CDK4 and CyclinD1 expression while upregulating P21. Autophagy agonist-1 promotes the accumulation of autophagosomes and the proteins LC3 and PINK1, enhancing autophagy and mitophagy in HepG2 cells .
    Autophagy agonist-1
  • HY-201330
    CDK-IN-18

    		CDK Cancer
    CDK-IN-18 (Compound EX.161) is an orally active, brain-penetrant and selective inhibitor of CDK2, CDK4, and CDK6. CDK-IN-18 inhibits the activity of cyclin-CDK complexes, blocks phosphorylation of the retinoblastoma protein (pRb), arresting the cell cycle transition from G1 to S phase. CDK-IN-18 is promising for research of cancers, such as breast cancer (especially hormone receptor-positive, HER2-negative type), lung cancer, and colorectal cancer .
    CDK-IN-18
  • HY-W025074
    BML-278

    		Sirtuin Histone Methyltransferase Cancer
    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 cell cycle 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 .
    BML-278
  • HY-159609
    PROTAC GSPT1 degrader-1

    		PROTACs Cancer
    PROTAC GSPT1 degrader-1 (Compound F) is a PROTAC degrader for G1 to S phase transition protein 1 (GSPT1) that degrades GSPT1 with a rate of 95% (1 μM) GSPT1 and 86% (0.1 μM). PROTAC GSPT1 degrader-1 inhibits the cell viability of HL-60 with an IC50 of 9.2 nM. (Pink: ligand for target protein (HY-W599025); Black: linker (HY-159619); Blue: ligand for E3 ligase (HY-W087383))
    PROTAC GSPT1 degrader-1
  • HY-135564A
    RK-682

    		Phosphatase Phospholipase HIV Protease ERK Autophagy Infection Cancer
    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 cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24 .
    RK-682
  • HY-164411
    KRC-00715

    		c-Met/HGFR Cancer
    KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models .
    KRC-00715
  • HY-170405
    YB-3–17

    		PROTACs mTOR Cancer
    YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC50=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC50=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC50 of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))
    YB-3–17
  • HY-153803
    GBD-9

    		PROTACs Molecular Glues Btk Cancer
    GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) .
    GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).
    GBD-9
  • HY-135564
    RK-682 hemicalcium

    		Phosphatase Phospholipase HIV Protease ERK Autophagy Infection Cancer
    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 cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24 [2] .
    RK-682 hemicalcium
  • HY-174302
    PIM-1/HDAC-IN-2

    		Pim HDAC PARP Apoptosis Cancer
    PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].
    PIM-1/HDAC-IN-2
  • HY-159122
    CA IX-IN-2

    		Carbonic Anhydrase Reactive Oxygen Species (ROS) Apoptosis Cancer
    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 cell cycle 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 .
    CA IX-IN-2
  • HY-145849
    VEGFR2-IN-1

    		VEGFR Cancer
    VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition .
    VEGFR2-IN-1

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