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Results for "

G1/S transition

" in MedChemExpress (MCE) Product Catalog:

22

Inhibitors & Agonists

3

Peptides

1

Natural
Products

1

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13650
    Indisulam
    10+ Cited Publications

    E 7070

    		 Molecular Glues Carbonic Anhydrase Cancer
    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 cell cycle. 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 .
    Indisulam
  • HY-13817
    IU1
    Maximum Cited Publications
    25 Publications Verification

    		 Deubiquitinase Autophagy Apoptosis Cardiovascular Disease Neurological Disease Endocrinology Cancer
    IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .
    IU1
  • HY-B1165
    Cyproheptadine (hydrochloride sesquihydrate)
    3 Publications Verification

    		 p38 MAPK Checkpoint Kinase (Chk) Histamine Receptor 5-HT Receptor CDK PARP Apoptosis Cancer
    Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia .
    Cyproheptadine (hydrochloride sesquihydrate)
  • HY-P1726
    MSG606

    		Melanocortin Receptor Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    MSG606 is a selective melanocortin 1 receptor (MC1R) antagonist. MSG606 can abolish the neuroprotective effects of BMS-470539 (HY-15616) (MC1R agonist). MSG606 can inhibit cancer cell proliferation and transition from the G1 to the S phase. MSG606 can delay pain hypersensitivity and reduce cholesterol levels. MSG606 can be used for the researches of cancer, inflammation, neurological and metabolic disease, such as breast cancer and subarachnoid hemorrhage (SAH) .
    MSG606
  • 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-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-103333
    Arvanil

    N-Vanillylarachidonamide

    		 TRP Channel Cannabinoid Receptor CD74 Akt Orexin Receptor (OX Receptor) Neurological Disease Inflammation/Immunology
    Arvanil (N-Vanillylarachidonamide) is a mixed agonist of CB1 and TRPV1 receptors. Arvanil downregulates CD25, HLA-DR, CD134/OX40, blocks G1/S phase transition, and induces phosphorylation of Akt. Arvanil does not induce apoptosis in cells. Arvanil inhibits lymphocyte activation and ameliorates autoimmune encephalomyelitis. Arvanil can be used in research related to Huntington's disease, vomiting, and multiple sclerosis .
    Arvanil
  • 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-201330
    GDC-4198

    RGT-419B

    		 CDK Cancer
    GDC-4198 (RGT-419B) is an orally active CDK4/2 inhibitor with desired degrees of selectivity against kinases such as CDK6, CDK9 and GSK3β. GDC-4198 inhibits the activity of cyclin-CDK complexes, blocks phosphorylation of the retinoblastoma protein (pRb), arresting the cell cycle transition from G1 to S phase. GDC-4198 is promising for research of cancers, such as breast cancer (especially hormone receptor-positive, HER2-negative type), lung cancer, and colorectal cancer .
    GDC-4198
  • HY-176128
    BWA-6047

    		PROTACs Androgen Receptor Apoptosis PARP Caspase Cancer
    BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC50 values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .
    BWA-6047
  • HY-175810
    GSPT1 degrader-8

    		Molecular Glues Cancer
    GSPT1 degrader-8 is a potent and orally active G1 to S phase transition 1 (GSPT1) molecular glue degrader. GSPT1 degrader-8 induces GSPT1 degradation and inhibits tumor growth. GSPT1 degrader-8 can be used for the research of cancer, such as breast cancer .
    GSPT1 degrader-8
  • HY-13650R
    Indisulam (Standard)

    E 7070 (Standard)

    		 Molecular Glues Carbonic Anhydrase Reference Standards Cancer
    Indisulam (Standard) is the analytical standard of Indisulam. This product is intended for research and analytical applications. 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 cell cycle. 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 .
    Indisulam (Standard)
  • HY-114338B
    Dalpiciclib isethionate

    SHR-6390 isethionate

    		 CDK Cancer
    Dalpiciclib (isethionate) is a CDK4/6 inhibitor. Dalpiciclib (isethionate) inhibits the kinase activity of CDK4 and CDK6, thereby blocking the G1-to-S phase transition of the cell cycle and suppressing abnormal cell proliferation. Dalpiciclib (isethionate) can be used for the study of breast cancer .
    Dalpiciclib isethionate
  • HY-159609
    GSPT1 degrader-9

    		Molecular Glues Cancer
    GSPT1 degrader-9 (Compound F) is a cereblon-based molecular glue 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). GSPT1 degrader-9 inhibits the cell viability of HL-60 with an IC50 of 9.2 nM .
    GSPT1 degrader-9
  • HY-177766
    GSPT1 degrader-17

    		Molecular Glues Apoptosis Cancer
    GSPT1 degrader-17 (Compound 9q) is a potent and selective cereblon-based molecular glue degrader that targets G1 to S phase transition 1 (GSPT1). GSPT1 degrader-17 degrades GSPT1 in U937 cells with a DC50 of 35 nM and Dmax of 81.65%. GSPT1 degrader-17 has a strong inhibitory effect on U937, MOLT-4 and MV4-11 cells with IC50 values of 0.019, 0.006 and 0.027 μM. GSPT1 degrader-17 can induce cells apoptosis and G0/G1 phase arrest. GSPT1 degrader-17 can be used for the research of cancer, such as acute myeloid leukemia .
    GSPT1 degrader-17
  • HY-177724
    GSPT1 degrader-11

    		Molecular Glues Cancer
    GSPT1 degrader-11 is a CRBN-dependent G1 to S phase transition 1 (GSPT1) molecular glue degrader (DC50 = 67.7 nM, Dmax = 97%). GSPT1 degrader-11 can inhibit MDA-MB-231 CRBN-WT cells proliferation (IC50 = 2.07 μM). GSPT1 degrader-11 can be used for the research of cancer .
    GSPT1 degrader-11
  • HY-177765
    GSPT1 degrader-16

    		Molecular Glues Cancer
    GSPT1 degrader-16 (Compound Lib-B-18J) is a potent and selective cereblon-based molecular glue degrader that targets G1 to S phase transition 1 (GSPT1). GSPT1 degrader-16 shows inhibitory effect to RS4;11, Molt4, and MM.1S cells with IC50 values of 0.002, 0.26 and 0.37 μM. GSPT1 degrader-16 can be used for the research of cancer, such as acute lymphoblastic leukemi .
    GSPT1 degrader-16
  • HY-P1726A
    MSG606 TFA

    		Melanocortin Receptor Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    MSG606 TFA is a selective melanocortin 1 receptor (MC1R) antagonist. MSG606 TFA can abolish the neuroprotective effects of BMS-470539 (HY-15616) (MC1R agonist). MSG606 TFA can inhibit cancer cell proliferation and transition from the G1 to the S phase. MSG606 TFA can delay pain hypersensitivity and reduce cholesterol levels. MSG606 TFA can be used for the researches of cancer, inflammation, neurological and metabolic disease, such as breast cancer and subarachnoid hemorrhage (SAH) .
    MSG606 TFA
  • HY-159610
    GSPT1 degrader-10

    		Molecular Glues Cancer
    GSPT1 degrader-10 (compound A) is a cereblon-based molecular glue degrader of GSPT1 with more than 95% degradation. GSPT1 degrader-8 inhibits cell viability in HL-60 cells with an IC50 of 10 nM .
    GSPT1 degrader-10
  • HY-P4979
    Cdc25A (80-93) (human)

    		Biochemical Assay Reagents Cancer
    Cdc25A (80-93) (human) is a polypeptide that controls the cell proliferation and tumorigenesis by a change in expression of proteins involved in cyclin D1 regulation and G1/S transition. Cdc25A (80-93) (human) can be used in cancer research .
    Cdc25A (80-93) (human)
  • 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-164184
    Ly101-4B

    		Apoptosis Caspase HSP Early 2 Factor (E2F) DNA/RNA Synthesis Cancer
    Ly101-4B is an apoptosis inducer and multi-target inhibitor with antiproliferative, antitumor and cycytotoxic effects. Ly101-4B reduces HSF1 expression, inhibits microRNA-214 synthesis, downregulates HSP27, HSP70 and HSP90 expression, while suppressing E2F-dependent transcriptional activity and downregulating its target genes. Ly101-4B induces caspase 3/7-mediated apoptosis by reducing DNA synthesis, inhibiting the cell cycle and G1/S phase transition, without affecting RNA synthesis or inducing necrosis. Ly101-4B is selective for pancreatic ductal adenocarcinoma cells with different genotypes and varying degrees of E2F dependence. Ly101-4B can be used in research related to epithelial ovarian cancer and pancreatic ductal adenocarcinoma .
    Ly101-4B

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