37

37 Publications Verification

Target:

PROTACs Epigenetic Reader Domain c-Myc Polo-like Kinase (PLK) CDK JAK STAT Pim Bcl-2 Family PAK Wnt β-catenin Caspase PARP Apoptosis Reactive Oxygen Species (ROS)

Research Areas:

Neurological Disease Cancer

ARV-825 is a BET protein PROTAC degrader that recruits cereblon, and it targets BRD2, BRD3, and BRD4 for degradation via the ubiquitin-proteasome pathway. ARV-825 downregulates c-MYC, PLK1, MYCN, CDK4/6, JAK2, pSTAT3/5, PIM1, and Bcl-xL, upregulates p21 and p27, and modulates H3K27Ac-mediated transcription, the G2/M checkpoint, the Wnt/β-catenin pathway, and amino acid transport pathways. ARV-825 induces G1 phase cell cycle arrest, caspase 3/PARP-mediated apoptosis, DNA damage, and reactive oxygen species (ROS) production, reduces mitochondrial respiration, and simultaneously inhibits cell proliferation, clonogenic growth, and cell migration. ARV-825 is used in research on gastric cancer, leukemia, neuroblastoma, and cholangiocarcinoma .

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27

Berzosertib

27 Cited Publications

Cat. No.: HY-13902

CAS No.: 1232416-25-9

Purity: 99.70%

Synonyms: VE-822; VX-970; M6620

Target:

ATM/ATR Apoptosis STING Caspase

Research Areas:

Infection Metabolic Disease Cancer

Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib blocks ATR kinase activity, abrogates G₂/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .

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27

Berzosertib hydrochloride

27 Cited Publications

Cat. No.: HY-13902A

CAS No.: 1428935-04-9

Synonyms: VE-822 hydrochloride; VX-970 hydrochloride; M6620 hydrochloride

Target:

ATM/ATR Apoptosis STING Caspase

Research Areas:

Neurological Disease Cancer

Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib hydrochloride blocks ATR kinase activity, abrogates G₂/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib hydrochloride induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib hydrochloride can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .

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11

Mirin

11 Cited Publications

Cat. No.: HY-19959

CAS No.: 1198097-97-0

Target:

ATM/ATR Apoptosis

Research Areas:

Cancer

Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC₅₀=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells .

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GNE-900

Cat. No.: HY-15883

CAS No.: 1200126-26-6

Purity: 99.21%

Target:

Checkpoint Kinase (Chk) Apoptosis

Research Areas:

Cancer

GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC₅₀s of 0.0011, 1.5 μM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. Gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .

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WEE1-IN-13

Cat. No.: HY-178190

Target:

Wee1

Research Areas:

Cancer

WEE1-IN-13 (Compound 10) is a highly selective WEE1 kinase inhibitor (IC₅₀=0.7 nM). WEE1-IN-13 abrogates the G2/M checkpoint and induces tumor cell apoptosis. WEE1-IN-13 is promising for research of solid tumors (e.g., non-small cell lung cancer, ovarian cancer) .

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PLK1-IN-4

Cat. No.: HY-146792

CAS No.: 2622273-55-4

Target:

Polo-like Kinase (PLK)

Research Areas:

Cancer

PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC₅₀ < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma .

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Guanazole

Cat. No.: HY-W015940

CAS No.: 1455-77-2

Target:

DNA/RNA Synthesis

Research Areas:

Infection Cancer

Guanazole is a ribonucleotide reductase (RNR) inhibitor that blocks replicative DNA synthesis by inhibiting deoxyribonucleotide biosynthesis. Guanazole selectively inhibits DNA synthesis in rapidly proliferating tissues, induces replication stress and G2/M phase arrest in Schizosaccharomyces pombe, and exhibits myelosuppressive, immunosuppressive, and anti-L1210 leukemia activities. Guanazole does not induce DNA repair and only shows slight mutagenicity towards Salmonella typhimurium TA102. Guanazole serves as an alternative tool to Hydroxyurea (HY-B0313) for replication checkpoint studies in Schizosaccharomyces pombe. Guanazole can be applied in research related to leukemia and solid tumors .

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Isogranulatimide

Cat. No.: HY-112347

CAS No.: 244148-46-7

Target:

Checkpoint Kinase (Chk)

Research Areas:

Cancer

Isogranulatimide is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC₅₀ value of 0.1 μM. Isogranulatimide inhibits the G2/M checkpoint and inhibits the growth of p53-mutant tumor cells. Isogranulatimide is promising for research of tumors associated with DNA damage response .

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ST045945

Cat. No.: HY-156916

CAS No.: 93326-70-6

Target:

Microtubule‐associated serine/threonine kinase (MAST)

Research Areas:

Metabolic Disease

WAY-230563 (ST045945) is a serine/threonine kinase inhibitor that can block CHK1/CHK2-mediated cell cycle checkpoints. WAY-230563 can induce G2/M phase arrest and DNA damage in tumor cells .

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WEE1-IN-14

Cat. No.: HY-178150

CAS No.: 2803921-87-9

Target:

Wee1

Research Areas:

Cancer

WEE1-IN-14 (Compound 14) is a selective WEE1 inhibitor (IC₅₀: 0.5 nM in L-RB-FEP calculations, 1.0 nM in ADP-Glo kinase assay). Inhibition of Wee1 in cancer cells disrupts the G2-M checkpoint, removes the regulatory controls on the cell cycle, and leads to early onset of mitotic failure followed by apoptosis of tumor cells. Therefore, WEE1-IN-14 is a useful tool for studying cancer biology .

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