deficient

5,6-Dihydrouracil (5,6-Dihydrouracil) is an intermediate breakdown product of uracil.

ML604440 is a cell permeable proteasome β1i (LMP2) subunit inhibitor.

AZD-9574 is a selective inhibitor of PARP1 at the sites of SSBs. AZD-9574 exhibits anti-cancer activities and can be used in studies about HRD+ breast cancer and advanced solid malignancies.

Necrostatin 2 is a necrotic protein and receptor-interacting protein kinase 1 (RIPK1) inhibitor used to study inner ear disorders such as sudden deafness, dizziness and tinnitus.

Necrostatin-5 (Nec-5) is a selective RIP1 kinase inhibitor and cell necrosis inhibitor that prevents the death of Fadd-deficient Jurkat cells treated with TNF-α, with an EC50 of 240 nM.

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. It specifically inhibits RAD52-dependent single-chain annealing (SSA) and D-loop formation, with IC50 values of 5 µM and 8 µM, respectively. D-I03 also inhibits the growth of BRCA1 and BRCA2 deficient cells and prevents the formation of damage-induced RAD52 foci, but does not affect RAD51 foci induced by Cisplatin.

I-OMe-Tyrphostin AG 538 is a specific IGF-1R inhibitor and ATP-competitive inhibitor of PI5P4Kα (IC50: 1 µM).I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and exhibits preferential cytotoxicity to nutrient-deficient PANC1 cells.

Rufigallol (AI3-00865) is an electron-deficient disk-shaped molecule with six hydroxyl groups and is a good unit for inducing the formation of DLC from non-planar AIE molecules, an anthraquinone derivative.Rufigallol induces the acquisition of DLC properties, while the introduction of TPE groups gives the molecular structure good fluorescence in the aggregated state.The remarkable synergistic in vitro antimalarial effect, in vivo with vitamin C and ketones was synergistic and showed antimalarial activity.

Rhizoferrin TFA is a protein secreted by Legionella pneumophila that is an iron carrier and can induce cytokine production, promote Fe(3+) uptake by wild-type Legionella pneumophila, and promote the growth of iron-deficient bacteria.

α-(difluoromethyl)-DL-Arginine (RMI 71897) is an enzyma-activated, irreversible inhibitor of arginine decarboxylase for E. coli (Ki = 800 μM), Pseudomonas aeruginosa, and Klebsiella pneumoniae. At 0.01 mM, it has been shown to prevent osmotic stress-induced increases in arginine decarboxylase activity and putrescine synthesis in oat leaf cells. When combined with a variety of polyamine analogues, α-(difluoromethyl)-DL-Arginine inhibited the growth of Trypanosoma Crui in mammalian host cells at a minimum concentration of 10 mM and prevented the growth of Trypanosoma Crui in T-cell receptor alpha-deficient mouse models.

1,4-D-Gulonolactone (D-Gulonic acid γ-lactone) (also known as reduced ascorbic acid, RAA) is the substrate of the enzyme L-gulono-1,4-lactone oxidoreductase (EC 1.1.3.8), which catalyzes the last step of the biosynthesis of L-ascorbic acid (vitamin C) in plants and animals. The enzyme L-Gulono-1,4-lactone oxidase is missing in scurvy-prone, vitamin C-deficient animals, such as humans. 1,4-D-Gulonolactone is present in human blood and has been used as one of the markers to compare changes in exercise-induced oxidative stress.

VU0285655-1(BML-280) is a potent and selective phospholipase D2 (PLD2) inhibitor that inhibits the proliferation of PLD2-deficient cells.VU0285655-1 has an inhibitory effect on high glucose-induced caspase-3 cleavage and reduction of cell viability.VU0285655-1 is used in the study of diabetic retinopathy.

LY88074 Methyl ether is effective in inhibiting conditions associated with estrogen deprivation syndrome, such as osteoporosis and hyperlipidemia, which occur due to various estrogen-deficient states.

2'-O-Methyladenosine, a methylated adenine residue, is present in the urine of both normal individuals and patients with adenosine deaminase deficiency, and exhibits unique hypotensive activities.

AGI-24512 is a potent inhibitor of methionine adenylyltransferase 2α (MAT2A) (IC50: 8 nM).AGI-24512 shows antiproliferative activity in MTAP-deficient cancer cells.AGI-24512 inhibits MAT2A, which causes DNA damage in MTAP, and is often used in conjunction with anticancer compounds in cancer research.

RS-246204 is an R-spondin-1 substitute compound capable of initiating and sustaining intestinal organoids in R-spondin-1-deficient media, activating R-spondin-dependent pathways in DSS-induced colitis models, and promoting regeneration of damaged intestinal epithelium.

AB25583 is a potent inhibitor of the Polθ helicase domain (Polθ-hel). It blocks MMEJ repair, leading to DNA damage accumulation and synthetic lethality in BRCA1/2-deficient cancer cells.

KL-50, a selective toxin, effectively targets tumors deficient in the DNA repair protein O6-methylguanine-DNA-methyltransferase (MGMT), which corrects O6-alkylguanine lesions. This compound induces both DNA damage response pathways and cell cycle arrest in MGMT-deficient cells, regardless of mismatch repair (MMR) status. KL-50 shows promise in the study of brain tumors lacking MGMT.

Nic-15 (compound 4n) serves as an anti-constrictive agent targeting the low vascular characteristics of pancreatic tumors. These characteristics enable cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop resistance to treatment. Nic-15 modulates the PI3K/Akt/mTOR pathway and alleviates ER stress induced by Gemcitabine. It significantly inhibits migration and colony formation in MIA PaCa-2 and PANC-1 pancreatic cancer cells. When used in combination with Gemcitabine, Nic-15 effectively addresses resistance issues in pancreatic tumors. In xenograft models in vivo, Nic-15 notably enhances the efficacy of Gemcitabine.

H3B-616, as a powerful allosteric inhibitor of Carbamoyl phosphate synthetase 1 (CPS1) with an IC50 of 66 nM, targets CPS1, identified as a potential synthetic lethal target in LKB1-deficient non-small cell lung cancer. This overexpression of CPS1 facilitates pyrimidine synthesis in these cancer cells.

UNC10142 is a small-molecule antagonist of CHD1 (IC₅₀ = 1.7 μM). UNC10142 induces dose-dependent reduction in the viability of PTEN-deficient prostate cancer cells.

MU147 is an MRE11 nuclease inhibitor and chemical probe with anticancer properties, exhibiting lethal effects on Ehrlich ascites tumor cells both in vivo and in vitro. It disrupts the MRE11 nuclease-dependent double-strand break repair mechanism without impairing ATM activation. Additionally, MU147 damages the degradation of nascent strands at stalled replication forks and selectively affects BRCA2-deficient cells.

MU1409 is an MRE11 nuclease inhibitor with an IC50 of 12.1 μM. It also inhibits FEN1 and EXO1, with IC50 values of 24.2 μM and 176.4 μM, respectively. MU1409 impacts cellular DNA repair and prevents the degradation of stalled replication forks in BRCA2-deficient cells, making it a promising candidate for studying BRCA2 mutation-induced cancers.

SMD-3236 is a PRAOTAC degrader targeting SMARCA2, designed using SMARCA ligand and VHL-1 ligand, and exhibits prolonged anti-tumor activity in vivo. SMARCA2 acts as a synthetic lethal target in cancer cells lacking SMARCA4, with SMD-3236 showing 2000-fold selectivity for SMARCA2 over SMARCA4, having a DC50 of less than 1 nM and a Dmax of over 95%. In the human cancer xenograft models deficient in SMARCA4, notably the H838 model, SMD-3236 effectively induces loss of SMARCA2 in tumor tissue while sparing the SMARCA4 protein, thereby inhibiting tumor growth. The compound consists of a target protein ligand (red part) SMI-1074, a PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate, and an E3 ligase ligand (blue part) SMARCA2 ligand-14, forming the E3LigaseLigand-linker Conjugate 159.