tmz

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.

L189 is a human DNA ligase inhibitor, inhibits hLigI/III/IV (IC50: 5/9/5 μM).

MMC(TMZ)-TOC TFA exhibits high binding affinity and selectivity for the somatostatin receptor subtype 2 (SSTR2). It targets the delivery of TMZ to SSTR2-positive tumor cells, making MMC(TMZ)-TOC TFA useful for cancer research.

MMC(TMZ)-TOC exhibits a high binding affinity and selectivity for somatostatin receptor subtype 2 (SSTR2). It is designed to target and deliver TMZ specifically to SSTR2-positive tumor cells. MMC(TMZ)-TOC is applicable for cancer research.

K-TMZ is a DNA alkylating agent. It increases the concentration of O6-methylated deoxyguanosine in U87 glioblastoma multiforme (GBM) cells in a concentration-dependent manner. K-TMZ reduces cell viability of GBM cell lines lacking (IC50s = 18-44 μM) or expressing O6-methylguanine DNA methyltransferase (MGMT; IC50s = 115-240 μM). K-TMZ can cross the blood-brain barrier and increases survival in a Br23c mouse xenograft model of GBM when administered at a dose of 14.9 mg/kg.

Temozolomide Acid (TMZA) is a metabolite of temozolomide (TMZ). Temozolomide processes anticancer activity in vitro. Temozolomide (TMZ) is an oral alkylating agent used to treat glioblastoma multiforme (GBM) and astrocytomas.

GNF362 is an orally available, selective and potent inhibitor of inositol trisphosphate 3'kinase B (ITPKB), inhibits Itpka and Itpkc, overcomes TMZ chemoresistance, and selectively deletes donor allogeneic reactive T-cells.GNF362 reverses the migratory stimulatory effects of ITPKA overexpression.

HedgehogIN-11 is an orally active Hedgehog inhibitor. It reduces resistance to Temozolomide (TMZ) by downregulating O6-methylguanine-deoxyribonucleotides methyltransferase (MGMT) expression through the Hedgehog pathway. HedgehogIN-11 significantly inhibits the migration and invasion of TMZ-resistant glioblastoma cells and induces apoptosis. Computational modeling predicts good blood-brain barrier penetration for HedgehogIN-11. This compound is applicable for glioblastoma (GBM) research.

MGMT-IN-1 (Compound 2) is a photoactivatable inhibitor of MGMT. It only effectively enhances the cytotoxicity of Temozolomide (TMZ) under light exposure, significantly increasing TMZ-induced DNA damage. MGMT-IN-1 is applicable for research in toe giant cell tumor.

MTIC is the active metabolite of Temozolomide (TMZ) with anticancer and antitumor activity and is used in the study of melanoma.3'-Sialyllactose (3'-SL) sodium is a prebiotic with anti-inflammatory activity.

PARP1-IN-10 (compound 12c) is a highly potent and non-cytotoxic PARP1 inhibitor with an in vitro IC50 value of 50.62 nM, effectively inducing cell cycle arrest at the G2/M phase and apoptosis, while significantly augmenting the cytotoxic effects of temozolomide (TMZ) [1].

GPI-15427 is a potent PARP-1 inhibitor capable of crossing the blood-brain barrier, which can significantly increased the antitumor activity of the methylating agent TMZ against malignant melanoma, glioblastoma multiforme, or lymphoma growing at the CNS site. GPI-15427 acts as a potent inhibitor of the enzyme, being capable of inhibiting the activity of purified PARP-1 at nanomolar concentrations. GPI-15427 induced significant sensitization to radiotherapy, representing a promising new treatment in the management of HNSCC.

PP5-IN-2, a selective and orally active inhibitor of protein phosphatase 5 (PP5), exhibits an IC 50 of 0.9 μM. This compound activates p53 and leads to the downregulation of cyclin D1 and MGMT, thereby inducing cell cycle arrest and reversing Temozolomide (TMZ) resistance in the U87 MG cell line. Additionally, PP5-IN-2 has demonstrated effective inhibition of tumor growth in the xenograft mouse model.