ionizing

Psoralidin inhibits Akt phosphorylation and phosphatidylinositol 3-kinase activation and transcriptionally. Psoralidin possesses anticancer and chemopreventive properties.

AZ 14145845, a potent and highly selective dual Mer/Axl kinase inhibitor (pIC50 = 7 nM and 7.8 nM in pAxl and pMer, respectively), demonstrates significant efficacy in reducing tumor growth in a dose-dependent manner within the Mer and Axl kinase Ba/F3 tumor xenograft model in vivo. When combined with anti-PD1 antibodies and ionizing radiation, this compound enhances survival rates in mice bearing MC38-derived tumors. Additionally, AZ 14145845 is orally bioavailable.

IRF1-IN-2 is a small molecule inhibitor of interferon regulatory factor 1 (IRF1) that functions by reducing the binding affinity of IRF1 for the caspase-1 (CASP1) gene promoter. this inhibition subsequently suppresses critical cell death signaling pathways, such as pyroptosis, and provides robust protection against ionizing radiation-induced skin inflammatory damage in preclinical models.

IRF1-IN-1 (Compound I-2) is an IRF1 inhibitor that reduces IRF1 recruitment to the Caspase 1 promoter, inhibiting the cleavage of Caspase 1, GSDMD, IL-1, and PARP1, thereby protecting against skin inflammatory damage.

STF-1084 is an inhibitor that cannot penetrate cells and targets ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (ENPP1) with an apparent Ki of 0.11 µM. It demonstrates selectivity for ENPP1 over ENPP2 and alkaline phosphatase (ALP) with apparent Kis of 5.5 and >100 µM, respectively, and does not affect a panel of 468 kinases at 1 µM. STF-1084 hinders the extracellular breakdown of cGAMP in ENPP1-overexpressing and cGAS-expressing 293T cells, with an IC50 of 0.340 µM, and enhances mRNA expression for the gene encoding IFN-β in CD14+ primary human peripheral blood mononuclear cells (PBMCs) when incubated with conditioned medium from ENPP1-overexpressing and cGAS-expressing 293T cells treated with STF-1084. In a live setting, STF-1084, when combined with ionizing radiation, elevates the proportion of tumor-associated CD11c+ cells among antigen-presenting cells (APCs) in a murine mammary cancer model (4T1).

K1586 is an effective guanidine derivative targeting Chk1. It enhances the degradation of Chk1, sensitizing colorectal cancer cells to ionizing radiation, and demonstrates anticancer activity.

dA-NHbenzylSCF 3 is a radiosensitizer characterized by its low toxicity to both cancerous and normal cells. However, it significantly enhances the destruction of cancer cells in the presence of ionizing radiation (IR). This compound promotes apoptosis by capturing electrons and inducing DNA double-strand breaks (DSBs). dA-NHbenzylSCF 3 is frequently utilized in research on cancers such as prostate and breast cancer.

ART5537 is a selective EXO1 inhibitor with an EC50 of 55 nM, an IC50 of 3.4 nM, and a Kd of 6.8 nM. It inhibits the homologous recombination (HR) process in HAP1 parental cells with an EC50 of 7.2 nM. The selectivity of ART5537 for the broad-spectrum nuclease superfamily members is over 200-fold higher. Its biological effects are entirely driven by EXO1 inhibition. ART5537 enhances sensitivity to ionizing radiation and exhibits synergism with Olaparib. It is applicable in research on breast and colon cancers.

Motexafin gadolinium, also known as PCI 0120, is a synthetic metallotexaphyrin with radiosensitizing and chemosensitizing properties. Motexafin gadolinium accumulates in tumor cells preferentially due to their increased rates of metabolism, generating rea

Potent Chk2 inhibitor (IC50 = 3 nM). Shows >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. Inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells. Blocks ionizing radiation-induced apoptosis of mouse thymocytes. Caldwell et al (2011) Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J.Med.Chem. 54 580 PMID:21186793

Valeryl-L-carnitine is a short-chain acylcarnitine and a derivative of L-carnitine . Valeryl-L-carnitine levels increase in the serum of rhesus monkeys following exposure to 7 and 10 Gray units (Gy) of ionizing radiation.[1]

XJB-5-131 is a synthetic, bi-functional antioxidant specifically designed to target mitochondria for the scavenging of reactive oxygen species (ROS) and electrons, thereby acting as a radical scavenger. Additionally, it serves as an effective protector and mitigator against ionizing irradiation for cord blood mononuclear cells (CB MNCs).

Tirapazamine (Win59075) is a potent cytotoxic agent under hypoxic conditions, can induce apoptosis by inducing breaks in single and double-stranded DNA, as well as chromosomal breaks. The compound sensitizes cells to other ionizing radiation and other cytotoxic agents like cisplatin.

SU-11752 is a potent and selective DNA-PK inhibitor. Inhibition kinetics and a direct assay for ATP binding showed that SU11752 inhibited DNA-PK by competing with ATP. SU11752 inhibited DNA double-strand break repair in cells and gave rise to a five-fold sensitization to ionizing radiation. At concentrations of SU11752 that inhibited DNA repair, cell cycle progression was still normal and ATM kinase activity was not inhibited.

Etanidazole (SR-2508) is a 2-nitroimidazole drug with radiosensitizing properties. Etanidazole depletes glutathione and inhibits glutathione transferase, thereby enhancing the cytotoxicity of ionizing radiation. This agent may also be useful as an imaging agent for identifying hypoxic, drug-resistant regions of primary tumors or metastases. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP +/- NU1085 (10 microM) for 72 h.

Reltecimod TFA (AB-103 TFA) is a CD28 (T-lymphocyte receptor) mimetic that acts as a CD28 antagonist, inhibiting the stimulation of t-cells by a range of bacterial pathogens thereby attenuating acute inflammation for the treatment of necrotizing soft tissue infections (NSTI).

2-Stearoyl-rac-glycerol is a natural product and monoglyceride, serving as an endogenous metabolite in mice and rats.

XRD-0394 is a highly effective and selective dual inhibitor of ATM and DNA-PKcs, exhibiting oral bioactivity. It notably increases tumor cell destruction both in vitro and in vivo when combined with therapeutic ionizing radiation. Furthermore, XRD-0394 enhances the efficacy of PARP and topoisomerase I inhibitors in vitro [1].

Niacinamide ascorbate is a vitamin complex that combines niacinamide (vitamin B3) and ascorbic acid (vitamin C). This compound is known to reduce the risks associated with exposure to ionizing radiation, including radiation-induced acute leukemia, breast cancer, thyroid cancer, and other somatic and genetic mutations.

Radretumab (also known as L19SIP) is a fully human monoclonal antibody in a small immunoprotein (SIP) format that specifically targets the extra-domain B (ED-B) of fibronectin. ED-B is a crucial marker of angiogenesis, highly expressed in the extracellular matrix of neovasculature within various solid tumors but nearly absent in normal adult tissues. Radretumab is typically labeled with radioisotopes such as 131I to deliver ionizing radiation directly to tumor sites through high-affinity binding to tumor vessels. In clinical trials, it is investigated for treating solid tumors and associated brain metastases.