ionizing

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.

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.

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

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.

IRF1-IN-1 (Compound I-2) is an IRF1 inhibitor that reduces IRF1 recruitment to the CASP1 promoter. It inhibits cell death signaling pathways by preventing the cleavage of Caspase 1, GSDMD, IL-1, and PARP1. Additionally, IRF1-IN-1 has a protective effect against ionizing radiation-induced skin inflammation.

IRF1-IN-2 (Compound I-19) is an inhibitor of IRF1. It reduces the recruitment of IRF1 to the CASP1 promoter and hinders cell death signaling pathways by inhibiting the cleavage of Caspase 1, GSDMD, IL-1, and PARP1, as well as by preventing the phosphorylation of TKB1. The compound also upregulates GPX4 and downregulates FACL4. Additionally, IRF1-IN-2 provides protective effects against skin inflammatory damage induced by ionizing radiation.

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

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).

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.

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

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]

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].

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).

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).

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.

2-Stearoyl-rac-glycerol, a monoacylglycerol with stearic acid at the sn-2 position, exhibits elevated levels in mouse plasma after low-dose ionizing radiation exposure and in rat kidney following ischemia-reperfusion injury models.