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pan-γH2AX

" in MedChemExpress (MCE) Product Catalog:

442

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13

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2

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2

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8

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2

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13

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11

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4

Click Chemistry

6

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-137843
    NSC 80467

    		DNA/RNA Synthesis Cancer
    NSC 80467, a DNA damaging agent, selectively inhibits survivin. NSC 80467 preferentially inhibits DNA synthesis and results in induction of γH2AX and pKAP1, two markers of DNA damage .
    NSC 80467
  • HY-147356
    ERCC1-XPF-IN-2

    		DNA/RNA Synthesis Cancer
    ERCC1-XPF-IN-2 is a potent ERCC1-XPF endonuclease inhibitor with an IC50 value of 0.6 μM. ERCC1-XPF-IN-2 shows activity in nucleotide excision repair, cisplatin enhancement and γH2AX assays .
    ERCC1-XPF-IN-2
  • HY-122181
    OTS186935
    4 Publications Verification

    		 Histone Methyltransferase Cancer
    OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
    OTS186935
  • HY-122181B
    OTS186935 hydrochloride
    4 Publications Verification

    		 Histone Methyltransferase Cancer
    OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
    OTS186935 hydrochloride
  • HY-N7271
    Solanidine
    1 Publications Verification

    		 RAD51 MDM-2/p53 Cardiovascular Disease Cancer
    Solanidine is an orally active cholestane alkaloid. Solanidine can be isolated from potato. Solanidine decreases RAD51 and increases γH2AX and p53. Solanidine has anti-tumor effects on LLC tumors and lung cancer. Solanidine promotes breast cancer cell proliferation. Solanidine reduces neovascularization. Solanidine causes abortion in some pregnant mice [2] .
    Solanidine
  • HY-172537
    Indolimine-214

    		DNA/RNA Synthesis Inflammation/Immunology Cancer
    Indolimine-214 is a metabolite of M. morganii Indolimine-214 increases the level of γH2AX in HeLa cells. Indolimine-214 can be used in the study of inflammatory bowel disease (IBD) and colorectal cancer (CRC) .
    Indolimine-214
  • HY-157954
    WRN inhibitor 6

    		DNA/RNA Synthesis Apoptosis Cancer
    WRN inhibitor 6 (compound 3ci) is a potent WRN inhibitor. WRN inhibitor 6 induces apoptosis. WRN inhibitor 6 increases the expression of p-p53, P-Chk2, γH2AX expression .
    WRN inhibitor 6
  • HY-121777
    SFOM-0046

    		DNA/RNA Synthesis Cancer
    SFOM-0046 arrests cell cycle in S-phase and causes DNA replication stress leading to the phosphorylation of H2AX into γ-H2AX. SFOM-0046 induces DNA damages. SFOM-0046 is a potent anticancer agent .
    SFOM-0046
  • HY-122181A
    OTS186935 trihydrochloride

    		Histone Methyltransferase Cancer
    OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
    OTS186935 trihydrochloride
  • HY-123786
    NSC745887

    		Apoptosis Caspase Cancer
    NSC745887 (compound 25) is an inhibitor that targets DNA topoisomerase cleavage, activates the caspase-8/9-caspase-3-poly (ADP-ribose) polymerase cascade, and induces apoptosis in cancer cells. NSC745887 enhances γH2AX expression and causes DNA fragmentation leading to DNA damage [2].
    NSC745887
  • HY-158166
    DNA-PK-IN-13

    		DNA-PK Inflammation/Immunology Cancer
    DNA-PK-IN-13 (Compound SK10) is a DNA-PK inhibitor that exhibits potent inhibitory activity (IC50= 0.11 nM). DNA-PK-IN-13 regulates tumor cell proliferation by decreasing the expression level of γH2A.X and enhancing the sensitivity of tumor cells to chemotherapeutic agents. DNA-PK-IN-13 is suitable for oncology studies .
    DNA-PK-IN-13
  • HY-168877
    FMP

    		MDM-2/p53 Reactive Oxygen Species (ROS) Apoptosis Caspase PARP Bcl-2 Family Cancer
    FMP is a Platinum(IV) complexe. FMP significantly upregulates the expression of γ-H2AX and p53. FMP increases the production of ROS. FMP markedly upregulates the expressions of Apoptosis-related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP shows antiproliferative activity against breast cancer .
    FMP
  • HY-171124
    Tilatamig samrotecan

    AZD9592

    		 Topoisomerase DNA/RNA Synthesis Cancer
    Tilatamig samrotecan (AZD9592) is an antibody-drug conjugate (ADC) used to deliver topoisomerase I inhibitors (TOP1i), targeting the epidermal growth factor receptor (EGFR) and c-MET, with anti-tumor activity. Tilatamig samrotecan (AZD9592) can induce DNA double-strand breaks, increase the expression of pRAD50 and γH2AX, and inhibit the growth of non-small cell lung cancer [2].
    Tilatamig samrotecan
  • HY-170937
    Urease-IN-20

    		Bacterial Apoptosis Reactive Oxygen Species (ROS) Infection
    Urease-IN-20 (compound XBP2) is an inhibitor of Helicobacter pylori (H. pylori). Urease-IN-20 inhibits H. pylori with an IC50 of 0.14 μM. Urease-IN-20 reduces cell Apoptosis and decreases ROS and γH2AX in GES-1 cells infected with H. pylori. Urease-IN-20 exhibits significant gastric mucosal protective effects. Urease-IN-20 shows the potential for H. pylori research .
    Urease-IN-20
  • HY-N7271R
    Solanidine (Standard)

    		Reference Standards RAD51 MDM-2/p53 Cardiovascular Disease Cancer
    Solanidine (Standard) is the analytical standard of Solanidine. This product is intended for research and analytical applications. Solanidine is an orally active cholestane alkaloid. Solanidine can be isolated from potato. Solanidine decreases RAD51 and increases γH2AX and p53. Solanidine has anti-tumor effects on LLC tumors and lung cancer. Solanidine promotes breast cancer cell proliferation. Solanidine reduces neovascularization. Solanidine causes abortion in some pregnant mice [2] .
    Solanidine (Standard)
  • HY-160005
    LMP517

    NSC 781517

    		 Topoisomerase DNA/RNA Synthesis Cancer
    LMP517 (NSC 781517) is a potent and non-camptothecin Topoisomerase I and II (TOP1 and TOP2) dual inhibitor. LMP517 can induce TOP1 and TOP2 cleavage complexes (TOP1ccs and TOP2ccs). LMP517 can induce cancer cells DNA damage and γH2AX production. LMP517 can be used for the research of cancer, such as small cell lung cancer [2].
    LMP517
  • HY-163942
    GSK_WRN4

    		DNA/RNA Synthesis Cancer
    GSK_WRN4 is an orally active WRN helicase inhibitor (pIC50=7.6). GSK_WRN4 induces DNA damage markers (p21, p-γH2AX, p-KAP1). GSK_WRN4 selectively inhibits microsatellite-unstable tumor growth in vitro and in vivo by inducing DNA double-strand breaks, particularly at expanded TA repeats and regions of DNA damage .
    GSK_WRN4
  • HY-122182
    OTS193320

    		Histone Methyltransferase Apoptosis Cancer
    OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .
    OTS193320
  • HY-117688
    WJ35435

    		HDAC Topoisomerase Apoptosis Cancer
    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 cell cycle 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 .
    WJ35435
  • HY-145289
    Antitumor agent-37

    		Apoptosis Cancer
    Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
    Antitumor agent-37
  • HY-145288
    Antitumor agent-36

    		Apoptosis Cancer
    Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
    Antitumor agent-36
  • HY-164802
    Pan-RAS-IN-7

    		Ras Cancer
    Pan-RAS-IN-7 (Compound D101) is a pan RAS inhibitor that can be used for the synthesis of ADCs. Pan-RAS-IN-7 can be utilized in cancer research .
    Pan-RAS-IN-7
  • HY-156555
    pan-KRAS-IN-3

    		Ras Cancer
    pan-KRAS-IN-3 (Example 84) is a pan-KRAS inhibitor. pan-KRAS-IN-3 can be used for research of cancers . pan-KRAS-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    pan-KRAS-IN-3
  • HY-175700
    YCJ-02

    		Topoisomerase Apoptosis Cancer
    YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC) .
    YCJ-02
  • HY-174431
    PAN endonuclease-IN-3

    		Endonuclease Influenza Virus Infection
    PAN endonuclease-IN-3 is a potent PAN endonuclease inhibitor that against influenza virus polymerase complexes with an IC50 of 17.4 nM. PAN endonuclease-IN-3 demonstrates potent inhibitory activities against PAN endonuclease. PAN endonuclease-IN-3 demonstrates robust antiviral activities against multiple current and different influenza virus strains while showing minimal cytotoxicity in MDCK cells. PAN endonuclease-IN-3 significantly suppresses viral replication in an A/WSN/33 infected mouse model.
    PAN endonuclease-IN-3
  • HY-168739
    Topoisomerase I inhibitor 17

    		Topoisomerase Reactive Oxygen Species (ROS) Apoptosis Survivin Bcl-2 Family IAP DNA/RNA Synthesis Cancer
    Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice .
    Topoisomerase I inhibitor 17
  • HY-172085
    SH514

    		IFNAR DNA/RNA Synthesis c-Myc CDK Cancer
    SH514 is an orally active IRF4 inhibitor (IC50 = 2.63 μM). SH514 binds to the IRF4-DBD domain, thereby inhibiting the interaction of IRF4 protein with DNA (KD = 1.28 μM). SH514 can inhibit the proliferation of IRF4-high-expressing NCI-H929 and MM.1R cells, and displays no cytotoxicity for normal cells. SH514 significantly downregulates the expression of IRF4 downstream target genes concentration-dependently. SH514 inhibits the expression of cell cycle-related proteins CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC in Multiple Myeloma cells. SH514 can induce DNA damage and increase the expression of γH2AX. SH514 effectively inhibits the proliferation of multiple myeloma tumors .
    SH514
  • HY-178032
    PARP1-IN-44

    		PARP Apoptosis Reactive Oxygen Species (ROS) DNA/RNA Synthesis STING Cancer
    PARP1-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC50 = 0.6 nM), and also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM). PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy .
    PARP1-IN-44
  • HY-163489
    pan-KRAS-IN-15

    		Ras Cancer
    pan-KRAS-IN-15 (compound 58) is a pan-KRAS inhibitor. pan-KRAS-IN-15 can be used in pancreatic cancer research .
    pan-KRAS-IN-15
  • HY-170785
    pan-KRAS-IN-17

    		Ras Cancer
    pan-KRAS-IN-17 (Example 34) is an inhibitor of pan KRAS .
    pan-KRAS-IN-17
  • HY-174433
    PAN endonuclease-IN-4

    		Influenza Virus Infection
    PAN endonuclease-IN-4 (Compound 41) is an inhibitor of PAN endonuclease with antiviral properties. PAN endonuclease-IN-4 is the prodrug of 39-(S). PAN endonuclease-IN-4 can significantly suppress viral replication in an A/WSN/33 infected mouse model .
    PAN endonuclease-IN-4
  • HY-101295
    Pan-RAS-IN-1
    5+ Cited Publications

    		 Ras Cancer
    Pan-RAS-IN-1 is a pan-Ras inhibitor that disrupts the interaction of Ras proteins and their effectors.
    Pan-RAS-IN-1
  • HY-163594
    Pan-RAS-IN-3

    		Ras Cancer
    Pan-RAS-IN-3 is a pan-Ras inhibitor, and can be used for study of melanoma and acute myeloid leukaemia .
    Pan-RAS-IN-3
  • HY-163147
    PAN endonuclease-IN-1

    		Influenza Virus Infection
    PAN endonuclease-IN-1 (Compound 23) is a potent PAN endonuclease inhibitor, with Kd values of 277 μM, 384 μM and 328 μM for WT, I38T and E23K PAN endonucleases, respectively. The RNA-dependent RNA polymerase acidic N-terminal (PAN) endonuclease, a critical component of influenza viral replication machinery, is an antiviral target .
    PAN endonuclease-IN-1
  • HY-176490
    pan-KRAS ligand 3

    		Ligands for Target Protein for PROTAC Ras Cancer
    Pan-KRAS ligand 3 is a pan-KRAS inhibitor. Pan-KRAS ligand 3 can be used for synthesis of PROTAC pan-KRAS degrader-1 (HY-176489) .
    pan-KRAS ligand 3
  • HY-164645
    pan-KRAS-IN-16

    		Ras Cancer
    pan-KRAS-IN-16 (Compound 3344) is an anti-RAS small molecule derived from an intracellular antibody fragment with pan-RAS-effector protein-protein interaction inhibitor properties. pan-KRAS-IN-16 binds to a hydrophobic pocket near to the effector-binding switch regions of RAS. pan-KRAS-IN-16 prevents endogenous RAS-dependent signaling in tumor cell lines .
    pan-KRAS-IN-16
  • HY-158028
    PAN endonuclease-IN-2

    		Influenza Virus Infection
    PAN endonuclease-IN-2 (compound T-31) is a PAN endonuclease inhibitor (IC50: 0.15 μM) and antiviral agent with broad-spectrum anti- Influenza activity. PAN is the N-terminal PA subunit of the polymerase-RNA complex and the dependent endonuclease (CEN) active site. PAN initiates RNA replication by promoting cleavage of the RNA strand and allowing the polymerase to begin synthesizing new RNA molecules. PAN endonuclease-IN-2 targets both the influenza HA and RdRp complexes, thereby interfering with viral entry into host cells and viral replication .
    PAN endonuclease-IN-2
  • HY-148098
    Pan KRas-IN-1
    1 Publications Verification

    		 Ras Cancer
    Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors .
    Pan KRas-IN-1
  • HY-175870
    pan-KRAS-IN-18

    		Ras Cancer
    pan-KRAS-IN-18 (Compound 14-1) is a pan-KRAS inhibitor. pan-KRAS-IN-18 has potent antitumor activities and significantly inhibits the proliferation of wild-type and mutant (such as KRAS G12D, KRAS G12V and KRAS G12C) cancer cells. pan-KRAS-IN-18 effectively inhibits tumor growth in GP2D and Panc0403 xenograft mouse models .
    pan-KRAS-IN-18
  • HY-163299
    pan-KRAS-IN-5

    		Ras Apoptosis PI3K Akt p38 MAPK Cancer
    pan-KRAS-IN-5 is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 strongly binds to and stabilizes KRAS rG4s, inhibits KRAS translation, and blocks the MAPK and PI3K-AKT pathways. pan-KRAS-IN-5 induces cell cycle arrest, prompts apoptosis in KRAS-driven cancer cells. pan-KRAS-IN-5 inhibits tumor growth and KRAS expression in KRAS-mutant xenograft. KRAS-IN-5 can be used for KRAS-driven cancer research .
    pan-KRAS-IN-5
  • HY-168671
    pan-KRAS ligand 1

    		Ligands for Target Protein for PROTAC Ras Cancer
    pan-KRAS ligand 1 is a Ligand for Target Protein for PROTAC. pan-KRAS ligand 1 can be used for synthesis PROTAC pan-KRAS degrader 4 (HY-168669) .
    pan-KRAS ligand 1
  • HY-162439
    pan-KRAS-IN-6

    		Ras Cancer
    pan-KRAS-IN-6 (compound 12) is a potent pan KRAS inhibitor with IC50 values of 9.79 nM (Kras G12D) and 6.03 nM (Kras G12V) .
    pan-KRAS-IN-6
  • HY-144676
    pan-HER-IN-1

    		EGFR Apoptosis Cancer
    pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan-HER inhibitor with IC50 values of 0.38, 1.6, 2.2 and 3.5 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and shows antitumor activities .
    pan-HER-IN-1
  • HY-144677
    pan-HER-IN-2

    		EGFR Apoptosis Cancer
    pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC50 values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities .
    pan-HER-IN-2
  • HY-158409
    Pan-RAS-IN-2

    		Molecular Glues Ras Cyclophilin Cancer
    Pan-rasin-2 (compound 6A) is a molecular glues that targets RAS. Pan-rasin-2 has significant inhibitory activity on cell proliferation of RAS mutant cell lines. Pan-rasin-2 can form ternary complexes with cyclophilin A (CYPA) and RAS (ON) proteins and the formation of ternary complexes can block the binding of RAF downstream of RAS, which has anti-tumor effects .
    Pan-RAS-IN-2
  • HY-156529
    pan-KRAS-IN-2

    		Ras Cancer
    pan-KRAS-IN-2 (Compound 6) is a pan-inhibitor with IC50s ≤ 10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A and Q61H); and an IC50 > 10 μM for KRAS G13D. pan-KRAS-IN-2 can be used to study various KRAS-mediated cancers, such as pancreatic cancer and colorectal cancer .
    pan-KRAS-IN-2
  • HY-144069
    Pan-Trk-IN-3

    		Trk Receptor Apoptosis Cancer
    Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC50 values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkA G595R, TrkA G667C, TrkA G667S, TrkA F589L and TrkC G623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis .
    Pan-Trk-IN-3
  • HY-176489
    PROTAC pan-KRAS degrader-1

    		PROTACs Ras Cancer
    PROTAC pan-KRAS degrader-1 is a pan-KRAS PROTAC degrader for degrading different KRAS mutation types, such as G12D, G12C, G12V, and G13D. PROTAC pan-KRAS degrader-1 potently degrades KRAS mutation (G12D) in AGS cells, with a DC50 of 1.1 nM, Dmax of 95%. PROTAC pan-KRAS degrader-1 can be used to search diseases caused by KRAS mutation or amplification, especially cancers such as breast cancer, bladder cancer, gastric cancer, etc . Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligase ligand (HY-170353); Black: linker (HY-176491);
    PROTAC pan-KRAS degrader-1
  • HY-10082
    Triapine
    5+ Cited Publications

    3-AP; pan-811; OCX191

    		 DNA/RNA Synthesis Cancer
    Triapine (3-AP; PAN-811) is a potent inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer.
    Triapine
  • HY-142452
    Pan-RAF kinase inhibitor 1

    		Raf Cancer
    Pan-RAF kinase inhibitor 1 is a potent inhibitor of Pan-RAF kinase. Pan-RAF kinase inhibitor 1 regulates MAPK signaling by inhibiting RAF kinase, thereby exerting an effect on the proliferation of RAS-mutant tumor cells. Pan-RAF kinase inhibitor 1 has the potential for the research of cancer diseases (extracted from patent WO2021110141A1, compound 16B) .
    Pan-RAF kinase inhibitor 1

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