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Pathways Recommended: Cell Cycle/DNA Damage
Results for "

Damage response

" in MedChemExpress (MCE) Product Catalog:

164

Inhibitors & Agonists

6

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4

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7

Peptides

4

Inhibitory Antibodies

22

Natural
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2

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7

Isotope-Labeled Compounds

1

Click Chemistry

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101566
    Elimusertib
    10+ Cited Publications

    BAY 1895344

    		 ATM/ATR Cancer
    Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity . Elimusertib can be used for the research of solid tumors and lymphomas .
    Elimusertib
  • HY-12484
    BMH-21
    10+ Cited Publications

    		 DNA/RNA Synthesis Cancer
    BMH-21 is a first-in-class DNA intercalator which inhibits RNA polymerase I (Pol I) transcription. BMH-21 possesses anticancer activity .
    BMH-21
  • HY-123834
    FEN1-IN-1
    5+ Cited Publications

    		 FLAP ATM/ATR Cancer
    FEN1-IN-1 (compound 1) is a small molecule flap endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg 2+ ions. FEN1-IN-1 initiaties a DNA damage response and activates the ATM checkpoint signalling pathway, the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is promising for research of cancers .
    FEN1-IN-1
  • HY-124293
    AA147
    4 Publications Verification

    		 ATF6 Reactive Oxygen Species (ROS) Neurological Disease Metabolic Disease
    AA147 is a endoplasmic reticulum (ER) proteostasis regulator. AA147 promotes protection against oxidative damage in neuronal cells and prevents endothelial barrier dysfunction by activating ATF6 arm (selectively) of the unfolded protein response (UPR) and the NRF2 oxidative stress response. AA147 can rebalances XBP1s expression in vivo, and also induces survival motor neuron (SMN) expression and spinal motorneuron (MN) protection .
    AA147
  • HY-112868B
    ABH hydrochloride
    1 Publications Verification

    		 Arginase NO Synthase Integrin Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    ABH (hydrochloride) is an orally active arginase inhibitor (Ki = 8.5 nM). ABH hydrochloride promotes NO production and reduces the expression of inflammatory response-related molecules (ICAM-1, VCAM-1, MCP-1). ABH hydrochloride improves erectile function, reduces lung damage, promotes wound healing, reduces arterial blood pressure, and improves vascular fibrosis .
    ABH hydrochloride
  • HY-P10408
    Candidalysin

    		EGFR MMP Calcium Channel NOD-like Receptor (NLR) ERK p38 MAPK Infection Inflammation/Immunology
    Candidalysin is a cytolytic peptide toxin secreted by the fungus Candida albicans. Candidalysin drives epithelial immune responses by activating the EGFR-MAPK signaling pathway, inducing MMP expression and calcium influx, and regulating the c-Fos transcription factor and MKP1 via p38 MAPK and ERK1/2 respectively. Candidalysin is essential for mucosal and systemic infections, activating NLRP3 to promote inflammatory responses, neutrophil recruitment, and Th17 immunity. Candidalysin activates LDH causing membrane damage and exhibiting cytotoxicity
    Candidalysin
  • HY-A0148A
    Halofantrine hydrochloride
    2 Publications Verification

    SKF-102886; WR-171669 hydrochloride

    		 Parasite Fungal Reactive Oxygen Species (ROS) Potassium Channel Infection
    Halofantrine hydrochloride (SKF-102886 hydrochloride; WR-171669 hydrochloride) is a blocker that delays the delayed rectifier potassium current by inhibiting human ERG channels, and it is a potent antimalarial agent with oral activity. Halofantrine hydrochloride inhibits the Cap1-dependent oxidative stress response of Candida albicans, suppresses ROS responses, and enhances the antifungal (Fungal) activity of oxidative damage agents. Halofantrine hydrochloride exhibits antifungal activity in the Galleria mellonella model, and shows antimalarial activity against Plasmodium strains both in vitro and in animal models. Halofantrine hydrochloride can be used in studies related to invasive candidiasis, falciparum malaria, and vivax malaria .
    Halofantrine hydrochloride
  • HY-112130
    AGI-24512
    2 Publications Verification

    		 Methionine Adenosyltransferase (MAT) Cancer
    AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC50 of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer .
    AGI-24512
  • HY-B0077
    Bendamustine hydrochloride
    5+ Cited Publications

    SDX-105

    		 DNA Alkylator/Crosslinker Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties .
    Bendamustine hydrochloride
  • HY-13567
    Bendamustine
    5+ Cited Publications

    SDX-105 free base

    		 DNA Alkylator/Crosslinker Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties .
    Bendamustine
  • HY-W010520
    Methylisothiazolinone

    		Environmental Pollutants MMP Bacterial Fungal Apoptosis Infection Inflammation/Immunology
    Methylothiazolinone is a bacterial and fungal inhibitor and preservative, as well as a sensitizer. Methylisothiazolinone can activate matrix metalloproteinases (MMPs) in human bronchial epithelial cells to induce apoptosis and inflammatory response. Methylisothiazolinone can promote the development of atopic dermatitis in mice by disrupting Th2/Th17 related immune responses. Methylisothiazolinone can cause mitochondrial damage in the endothelium of rat cerebral blood vessels .
    Methylisothiazolinone
  • HY-168162
    ZLC491

    		PROTACs CDK Cancer
    ZLC491 is an orally active PROTAC degrader that selectively targets CDK12/CDK13 and exhibits certain oral bioavailability. ZLC491 induces cereblon- and proteasome-dependent selective degradation of CDK12 and CDK13. ZLC491 inhibits the transcription and expression of long genes, and mainly acts on a subset of DNA damage response genes. ZLC491 inhibits the proliferation of various triple-negative breast cancer cells. ZLC491 can be used in research related to triple-negative breast cancer .
    ZLC491
  • HY-111940
    LUT014

    		Raf p38 MAPK ERK Inflammation/Immunology
    LUT014 is a topical inhibitor targeting BRAF that cannot pass through the blood-brain barrier. LUT014 inhibits BRAF kinase and abnormally activates the MAPK/ERK signaling pathway, promoting the proliferation of epidermal keratinocytes, repairing skin barrier damage caused by radiation damage, and alleviating inflammatory responses. LUT014 is independent of RAS signaling and accelerates the repair and regeneration of damaged skin cells. LUT014 can be used to study radiation dermatitis, especially skin damage caused by breast cancer radiotherapy .
    LUT014
  • HY-126020
    Bractoppin
    3 Publications Verification

    		 DNA/RNA Synthesis RAD51 Cancer
    Bractoppin is a potent and selective agent-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC50: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response .
    Bractoppin
  • HY-122198
    ML367
    1 Publications Verification

    		 Checkpoint Kinase (Chk) Cancer
    ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation .
    ML367
  • HY-101566A
    Elimusertib hydrochloride
    10+ Cited Publications

    BAY 1895344 hydrochloride

    		 ATM/ATR Cancer
    Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib hydrochloride has anti-tumor activity . Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas .
    Elimusertib hydrochloride
  • HY-N0754
    Eupalinolide A

    		YAP HSP Reactive Oxygen Species (ROS) ERK Autophagy Apoptosis Tyrosinase DNA/RNA Synthesis Neurological Disease Inflammation/Immunology Cancer
    Eupalinolide A is a Yes-associated protein (YAP) degrader and HSP70 inducer. Eupalinolide A inhibits osteogenic differentiation of tendon-derived stem cells (TDSCs). Eupalinolide A induces autophagy in hepatocellular carcinoma cells via activating the ROS/ERK signaling pathway. Eupalinolide A protects PAM212 cells from UVB-, Menadione (HY-B0332)-, or heat shock-induced apoptosis. Eupalinolide A alleviates trauma-induced heterotopic ossification (HO) of Achilles tendon and inhibits growth of MHCC97-L and HCCLM3 hepatocellular carcinoma xenograft tumors in mice. Eupalinolide A can be used for the study of traumatic heterotopic ossification of tendons and hepatocellular carcinoma .
    Eupalinolide A
  • HY-P2076
    Dusquetide

    SGX942

    		 p62 Bacterial Infection Cancer
    Dusquetide (SGX942) is a first-in-class innate defense regulator (IDR). Dusquetide modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide shows activity in both reducing inflammation and increasing clearance of bacterial infection . DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
    Dusquetide
  • HY-13703A
    Nimustine hydrochloride
    1 Publications Verification

    ACNU

    		 DNA Alkylator/Crosslinker DNA/RNA Synthesis Apoptosis p38 MAPK JNK AP-1 Cancer
    Nimustine hydrochloride (ACNU) is the hydrochloride salt form of Nimustine (HY-13703). Nimustine hydrochloride is an alkylating agent, which induces DNA double-strand breaks (DSBs) and inter-strand crosslinks (ICLs), thereby activating the DNA damage response (DDR) signaling pathway. Nimustine hydrochloride activates p38 MAPK/JNK signaling pathway, and exhibits antitumor activity .
    Nimustine hydrochloride
  • HY-144981
    HQ461
    1 Publications Verification

    		 CDK Molecular Glues Cancer
    HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death .
    HQ461
  • HY-114869
    DPQ
    3 Publications Verification

    		 PARP Neurological Disease Cancer
    DPQ is a selective PARP-1 inhibitor that blocks PARP-1-mediated DNA damage repair and NAD +/ATP consumption, thereby inhibiting excessive inflammatory responses. DPQ inhibits NF-κB pathway activation, reduces the expression of pro-inflammatory factors (such as TNF-α, IL-6) and oxidative stress. DPQ can be used in inflammation-related studies of acute lung injury, myocardial infarction, and neurodegenerative diseases .
    DPQ
  • HY-116217
    5-Fluoro-2'-deoxycytidine
    3 Publications Verification

    FdCyd; NSC-48006

    		 DNA Methyltransferase Cancer
    5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of thymidylate synthase inhibitor 5-fluoro-2′-dUMP. 5-Fluoro-2'-deoxycytidine can induce cell cycle arrest in tumor cells through the DNA damage response, and it has anti-tumor activity .
    5-Fluoro-2'-deoxycytidine
  • HY-137924
    JA2131
    1 Publications Verification

    		 Poly(ADP-ribose) Glycohydrolase (PARG) Cancer
    JA2131 is a small molecular inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG) (IC50=0.4 μM). JA2131 regulate DNA damage responses, causes replication fork stalling and cancer cell death .
    JA2131
  • HY-W010243
    Methylisothiazolinone hydrochloride

    		Bacterial MMP Apoptosis Fungal Infection Inflammation/Immunology
    Methylisothiazolinone hydrochloride is a bacterial and fungal inhibitor and preservative, as well as a sensitizer. Methylisothiazolinone hydrochloride can activate matrix metalloproteinases (MMPs) in human bronchial epithelial cells to induce apoptosis and inflammatory response. Methylisothiazolinone hydrochloride can promote the development of atopic dermatitis in mice by disrupting Th2/Th17 related immune responses. Methylisothiazolinone hydrochloride can cause mitochondrial damage in the endothelium of rat cerebral blood vessels .
    Methylisothiazolinone hydrochloride
  • HY-120084
    BTX161
    1 Publications Verification

    		 Casein Kinase Cancer
    BTX161, a thalidomide analog, is an effective CKIα degrader. BTX161 mediates human AML cell CKIα degradation more effectively than lenalidomide and activates the DNA damage response (DDR) and p53, while stabilizing p53 antagonist MDM2.
    BTX161
  • HY-138155
    NSC15520

    		DNA/RNA Synthesis Cancer
    NSC15520 is a small molecular inhibitor of Replication Protein A (RPA). NSC15520 specifically recognizes the RPA N-terminal DNA binding domain (DBD), and blocks the interaction of RPA with p53 or RAD9. NSC15520 also inhibtis helix destabilization of a duplex DNA (dsDNA) oligonucleotide, involves in DNA replication, DNA repair, DNA recombination, and DNA damage response signaling .
    NSC15520
  • HY-103316
    trans-Ned 19

    		Calcium Channel Cardiovascular Disease Inflammation/Immunology
    trans-Ned 19 is a NAADP antagonist and TPC blocker. trans-Ned 19 suppresses the calcium signal and the rat aorta relaxation in response to low histamine concentrations. trans-Ned 19 increases the spontaneous acrosome reaction rate, alleviates anti-CD3 mAb-induced intestinal inflammation, and improves kidney damage in mice with nephrotoxic serum nephritis .
    trans-Ned 19
  • HY-158345
    PROTAC ATM degrader-1

    		PROTACs ATM/ATR DNA/RNA Synthesis Apoptosis Cancer
    PROTAC ATM degrader-1 is a ATM PROTAC degrader with a KD value of 1.17 nM. PROTAC ATM degrader-1 triggers DNA damage response, cell cycle arrest, and apoptosis in cancer cells via the ubiquitin-proteasome-dependent degradation pathway. PROTAC ATM degrader-1 can be used for research on colorectal cancer .
    PROTAC ATM degrader-1
  • HY-153339
    E235

    		Eukaryotic Initiation Factor (eIF) Cancer
    E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research .
    E235
  • HY-N9487
    (R)-(-)-α-Phellandrene

    (-)-α-Phellandrene

    		 Environmental Pollutants Bacterial Infection Inflammation/Immunology
    (R)-(-)-α-Phellandrene ((-)-α-Phellandrene) is an the (R)-(-)-stereoisomer of α-phellandrene. α-phellandrene is an orally active cyclic monoterpene that attenuates inflammatory response, and induces DNA damage .
    (R)-(-)-α-Phellandrene
  • HY-P99928
    Efprezimod alfa

    MK 7110; CD24 Fc

    		 Transmembrane Glycoprotein Cancer
    Efprezimod alfa (MK 7110; CD24 Fc) is a humanized CD24-Fc fusion protein. Efprezimod alfa enhances the interaction between CD24 and Siglec-10, thereby regulating the response of innate immune cells to damage-associated molecular patterns, inhibiting the activation of antigen-presenting cells and subsequent inflammatory responses. Efprezimod alfa is applicable to the research of acute graft-versus-host disease and acquired immunodeficiency syndrome .
    Efprezimod alfa
  • HY-178208
    MDOLL-0286

    		Poly(ADP-ribose) Glycohydrolase (PARG) Cancer
    MDOLL-0286 is a selective Poly(ADP-ribose) Glycohydrolase (PARG) (ARH3) inhibitor with an IC50 of 2.3μM. MDOLL-0286 can inhibit ARH3’s poly-ADP-ribose hydrolytic activity on cellular substrates. MDOLL-0286 can inhibit DNA damage response. MDOLL-0286 can be used for the research of cancer .
    MDOLL-0286
  • HY-165084
    L-a-Phosphatidylserine sodium

    Soy PS sodium

    		 Liposome Inflammation/Immunology
    L-a-Phosphatidylserine sodium is an antigen targeting phosphatidylserine (PS) and can induce the production of polyclonal antibodies. L-a-Phosphatidylserine can trigger complement-dependent immune damage by binding to PS on the cell membrane surface. After L-a-Phosphatidylserine is recognized by antibodies, it activates the complement system, causing liposome membrane damage and content release, and then participates in the regulation of immune response and cell apoptosis signaling. L-a-Phosphatidylserine can be used in immunological research, such as antibody specificity analysis and complement activation mechanism research .
    L-a-Phosphatidylserine sodium
  • HY-W011425
    NTPO

    Nitrilotris(methylenephosphonic acid)

    		 Environmental Pollutants DNA Alkylator/Crosslinker MOFs Cancer
    NTPO (Nitrilotris methylenephosphonic acid) is a DNA damage inducer, causing genomic DNA damage and fragmentation, activating ATR-mediated cell cycle checkpoints. The DNA damaging effects of NTPO are abrogated by base excision repair (BER) but not nucleotide excision repair (NER) .
    NTPO
  • HY-W010243S
    Methylisothiazolinone-d3 hydrochloride

    		Isotope-Labeled Compounds Bacterial MMP Apoptosis Fungal Infection Inflammation/Immunology
    Methylisothiazolinone-d3 hydrochloride is the deuterium labeled Methylisothiazolinone hydrochloride (HY-W010243). Methylisothiazolinone hydrochloride is a bacterial and fungal inhibitor and preservative, as well as a sensitizer. Methylisothiazolinone hydrochloride can activate matrix metalloproteinases (MMPs) in human bronchial epithelial cells to induce apoptosis and inflammatory response. Methylisothiazolinone hydrochloride can promote the development of atopic dermatitis in mice by disrupting Th2/Th17 related immune responses. Methylisothiazolinone hydrochloride can cause mitochondrial damage in the endothelium of rat cerebral blood vessels .
    Methylisothiazolinone-d3 hydrochloride
  • HY-105017
    Evodenoson

    ATL 313; DE 112

    		 Adenosine Receptor Infection Inflammation/Immunology
    Evodenoson is a selective agonist of the A2A adenosine receptor. Evodenoson’s primary actions include reducing inflammatory responses, decreasing intestinal fluid secretion, edema, tissue damage, and neutrophil infiltration induced by Clostridium difficile toxin A. Evodenoson’s protective effect is achieved by reducing myeloperoxidase (MPO) and adenosine deaminase (ADA) activities, and by lowering the production of tumor necrosis factor-alpha (TNF-α) .
    Evodenoson
  • HY-135782
    iso-ADP ribose

    		Poly(ADP-ribose) Glycohydrolase (PARG) Cancer
    iso-ADP ribose is the small-molecule ligand for protein nucleic acid modification, comprising parts of two consecutive ADP-ribosyl units within the PAR chain. iso-ADP ribose specifically binds WWE, FHA and OB-fold domains, enabling PAR-dependent functional responses like ubiquitylation and supporting DNA damage signaling and repair. iso-ADP ribose can be used for cancer research .
    iso-ADP ribose
  • HY-W764758
    3-OH-Kynurenamine dihydroiodide

    		Aryl Hydrocarbon Receptor Inflammation/Immunology
    3-OH-Kynurenamine dihydroiodide is the dihydroiodide form of 3-OH-Kynurenamine (HY-156908). 3-OH-Kynurenamine dihydroiodide is an activator for aryl hydrocarbon receptor (AhR), and thus regulates the immune response. 3-OH-Kynurenamine dihydroiodide upregulates the expressions of Ido1 and Tgfb1, ameliorates the skin inflammation in psoriasis mouse model and kidney damage in nephrotoxic lupus mouse model .
    3-OH-Kynurenamine dihydroiodide
  • HY-164496
    KL-50

    		DNA/RNA Synthesis Cancer
    KL-50 is a selective toxin toward tumors that lack the DNA repair protein O 6-methylguanine-DNA-methyltransferase (MGMT), which reverses the formation of O 6-alkylguanine lesions. KL-50 activates DNA damage response pathways and cycle arrest in MGMT-cells, independent of mismatch repair (MMR). KL-50 is promising for research of brain tumors that lack the DNA repair protein MGMT .
    KL-50
  • HY-153190
    W1131
    1 Publications Verification

    		 Oxidative Phosphorylation STAT Ferroptosis Cancer
    W1131 is a potent STAT3 inhibitor, triggering ferroptosis. W1131 suppresses cancer progression in gastric cancer cell subcutaneous xenograft model, organoids model, and PDX model. W1131 effectively alleviates chemical resistance of cancer cells to 5-FU (HY-90006). W1131 regulates cell cycle, DNA damage response, and oxidative phosphorylation, including IL6-JAK-STAT3 pathway and ferroptosis pathway .
    W1131
  • HY-155801
    CRX 527

    		Toll-like Receptor (TLR) NF-κB TNF Receptor MyD88 Apoptosis DNA/RNA Synthesis Cardiovascular Disease Infection Neurological Disease Inflammation/Immunology Cancer
    CRX 527 is a TLR4 agonist. CRX 527 activates the MyD88-dependent, TRIF-dependent, and TRAF6/NF-κB signaling pathways downstream of TLR4, mimics lipid A, and regulates antigen processing and presentation by dendritic cells. CRX 527 stimulates innate immune responses and enhances vaccine efficacy. CRX 527 maintains the structural integrity of hematopoietic tissues, spleen and intestine, alleviates radiation-induced damage, preserves intestinal homeostasis, and inhibits apoptosis, inflammatory responses, oxidative stress and DNA damage. CRX 527 can be used in the research of acute radiation syndrome, melanoma, HPV-related tumors and intracerebral hemorrhage .
    CRX 527
  • HY-151883
    APE1-IN-2

    		Apoptosis MDM-2/p53 Cancer
    APE1-IN-2 (compound AP1) is a Pt(IV) proagent, targeting a critical BER protein, apurinic/apyrimidinic endonuclease 1 (APE1). APE1-IN-2 shows anticancer activity. APE1-IN-2 induces intracellular accumulation of platinum and activates DNA damage response and apoptosis signals .
    APE1-IN-2
  • HY-A0148
    Halofantrine

    SKF-102886 free base; WR-171669

    		 Parasite Fungal Potassium Channel Reactive Oxygen Species (ROS) Infection Cancer
    Halofantrine (SKF-102886 hydrochloride; WR-171669 hydrochloride) is a blocker that delays the delayed rectifier potassium current by inhibiting human ERG channels, and it is a potent antimalarial agent with oral activity. Halofantrine inhibits the Cap1-dependent oxidative stress response of Candida albicans, suppresses ROS responses, and enhances the antifungal (Fungal) activity of oxidative damage agents. Halofantrine exhibits antifungal activity in the Galleria mellonella model, and shows antimalarial activity against Plasmodium strains both in vitro and in animal models. Halofantrine can be used in studies related to invasive candidiasis, falciparum malaria, and vivax malaria .
    Halofantrine
  • HY-173059
    CDK12/13-IN-3

    		CDK Cancer
    CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6% .
    CDK12/13-IN-3
  • HY-146565
    DNA-PK-IN-8

    		DNA-PK Cancer
    DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin .
    DNA-PK-IN-8
  • HY-177780
    Cyclin K degrader 2

    		Molecular Glues CDK Apoptosis Cancer
    Cyclin K degrader 2 is a molecular glucose degrading agent that targets the cyclin K protein. Cyclin K degrader 2 has inhibitory activity against CDK1 and CDK9. Cyclin K degrader 2 causes a decrease in RNA polymerase II Ser2 phosphorylation levels, downregulation of DNA damage response gene expression, accumulation of DNA damage, G1 phase arrest of the cell cycle, and apoptosis. Cyclin K degrader 2 can be used for cancer research .
    Cyclin K degrader 2
  • HY-167917
    Conjugated linoleic acid

    		Drug Isomer Metabolic Disease Inflammation/Immunology Endocrinology Cancer
    Conjugated linoleic acid is a group of isomers of Linoleic acid (HY-N0729) containing conjugated double bonds. Conjugated linoleic acid is mainly derived from dairy products and ruminant meats. Conjugated linoleic acid exhibits various activities such as anti-carcinogenicity, immunomodulation, weight loss promotion, reduction of muscle damage, and alleviation of inflammatory responses. Conjugated linoleic acid can be used as a food additive .
    Conjugated linoleic acid
  • HY-135782A
    iso-ADP ribose TEA

    		Poly(ADP-ribose) Glycohydrolase (PARG) Cancer
    iso-ADP ribose TEA is the small-molecule ligand for protein nucleic acid modification, comprising parts of two consecutive ADP-ribosyl units within the PAR chain. iso-ADP ribose TEA specifically binds WWE, FHA and OB-fold domains, enabling PAR-dependent functional responses like ubiquitylation and supporting DNA damage signaling and repair. iso-ADP ribose TEA can be used for cancer research .
    iso-ADP ribose TEA
  • HY-144435
    ATR-IN-11

    		ATM/ATR Cancer
    ATR-IN-11 (Compound Hit01) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase. ATR kinase is a key regulating protein within the DNA damage response (DDR), responsible for sensing replication stress (RS). ATR-IN-11 is a promising lead compound for subsequent agent discovery targeting ATR kinase. ATR-IN-11 has the potential for the research of cancer disease .
    ATR-IN-11
  • HY-173273
    YJZ5118

    		CDK Apoptosis DNA/RNA Synthesis Akt Cancer
    YJZ5118 is a selective CDK12/CDK13 inhibitor with IC50 values of 39.5 nM and 26.4 nM. YJZ5118 suppresses transcription of DNA damage response genes and induces DNA damage in tumor cells. YJZ5118 inhibits proliferation and triggers apoptosis. YJZ5118 inhibits RNA polymerase II Ser2 phosphorylation and increases Akt pathway activity. YJZ5118 exhibits synergistic effects with Akt inhibitors. YJZ5118 can be used for the research of cancer, such as prostate cancer .
    YJZ5118

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