cisplatin

Cisplatin (CDDP) is a DNA cross-linking agent. Cisplatin has antitumor activity and inhibits DNA synthesis by forming DNA adducts in cancer cells. Cisplatin also activates ferroptosis and induces autophagy.

Cisplatin-resistant cells-IN-1 (Compound 8) exhibits high cytotoxicity against Cisplatin-resistant cells and effectively diminishes metabolic activity at low nanomolar concentrations, with an IC50 ranging from 0.14 to 1.79 μM in various resistant cell lines, including A549 A549-R, K562 K562-R, and MCF-7 MCF-7TamR [1].

Butein (2’,3,4,4’-tetrahydroxy Chalcone), a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit EGFR.

6-Methoxyflavanone (6-MeOF) is a positive allosteric modulator of the GABA response in human recombinant GABA A receptors, exhibiting antianxiety and anti-inflammatory properties, and is used to alleviate cisplatin-induced neuropathic pain.

Nitroaspirin (NCX 4016) is a nitric oxide donor and a nitro-derivative of Aspirin that inhibits cyclooxygenase. It induces cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells by down-regulating EGFR PI3K STAT3 signaling and modulating Bcl-2 family proteins. Additionally, Nitroaspirin possesses antithrombotic and antiplatelet properties and acts as a direct and irreversible inhibitor of COX-1.

PRLX-93936 HCL is an analog of erastin and demonstrated synergistic effects against non-small cell lung cancer (NSCLC) cells with cisplatin.

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.

(Rac)-AMXT-1501 4HCl is a polyamine transport inhibitor that inhibits polyamine transport and acts synergistically with cisplatin in HNSCC. (Rac)-AMXT-1501 4HCl has potential antimicrobial activity and inhibits neuroblastoma cell proliferation and pneumococcal pod biosynthesis by targeting ornithine decarboxylase and polyamine transport.

Zeniplatin (Zeniplatinum) is a new cisplatin complex with anticancer activity for the treatment of metastatic melanoma and kidney cancer.

monohydroxycisplatin is a useful organic compound for research related to life sciences. The catalog number is T68105 and the CAS number is 101311-26-6.

Carboplatin (JM-8) is a cisplatin derivative, a DNA synthesis inhibitor. Carboplatin binds to DNA, inhibits replication and transcription, and induces cell death. Carboplatin has antitumor activity.

Brusatol (NSC-172924) is a natural product isolated from the Brucea javanica plant. It inhibits Nrf2.

6-Aminonicotinamide (6-AN) is a well-established inhibitor of the NADP+-dependent enzyme.

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.

NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.

UTL-5g (3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl-) is a novel potential chemoprotective agent, TNF-α inhibitor that reduces cisplatin-induced side effects including nephrotoxicity, hepatotoxicity and hematotoxicity. It lowers elevated levels of AST, ALT, creatinine, BUN, and TNF-α, increases the reduced platelet count in mice, and acts as a novel chemo- and radioprotective agent.

Ondansetron hydrochloride dihydrate (GR 38032) is a competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.

Corilagin has anti-inflammatory activity. Corilagin has a significant antitumour potential and lower toxicity in normal cells in vitro.Corilagin can enhance the cytotoxicity of both cisplatin and doxorubicin on the Hep3B hepatoma cells.Corilagin has antiviral activity, reduces the cytotoxicity induced by EV71 or CA16 on Vero cells with and IC50 value of 5.6 and 32.33 μg/mL, respectively. Corilagin shows the potential to protect against HSV-1-induced encephalitis, and the beneficial effects may be mediated by inhibiting TLR2 signaling pathways.Corilagin has antifibrotics property and is potentiated in treating idiopathic pulmonary fibrosis(IPF), attenuates bleomycin-induced epithelial injury and fibrosis via inactivation of oxidative stress, proinflammatory cytokine release and NF-κB and TGF-β1 signaling. Solvent:Pyridine, Methanol, Ethanol, etc.

Eriodictyol-7-O-glucoside is an Nrf2 activator conferring protection against Cisplatin-induced toxicity. Eriodictyol-7-O-glucoside is a flavonoid and a free radical scavenger with antioxidant activity in pistachio skin.

CG347B is a selective inhibitor of HDAC6.

Eurycomalactone is a natural product isolated from Eurycoma longifolia Jack., acts as a potent NF-κB inhibitor( IC50 of 0.5 μM). Eurycomalactone inhibits protein synthesis, depletes cyclin D1, but does not affect TNFα-induced degradation of IκBα or the phosphorylation of IKKα β and IκBα.

RKS262 is a specific cyclin/CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several non-small cell lung cancer cell lines and few cell lines from other tissues were relatively resistant (GI(50) > 1 µM) to RKS262 treatment.

Difopein (TFA), a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein (TFA) leads to inductio

Nedaplatin (NSC-375101D) is a derivative of cisplatin and DNA damage agent for tumor colony forming units (IC50: 94 μM). Containing a novel ring structure in which glycolate is bound to the platinum by a bidentate ligand, nedaplatin forms reactive platinum complexes that bind to nucleophilic groups in DNA, resulting in intrastrand and interstrand DNA cross-links, apoptosis and cell death.

TDRL-X80 is a potent inhibitor of the pigmented dry skin protein (XPA), inhibiting the DNA binding activity of XPA. It acts on single, double, and cisplatin-damaged DNA with IC50 values of 18, 20, and 29 μM in fluorescence polarization (FP) assays and 21, 39, and 28 μM in ELISA assays.

(R)-Azasetron besylate (SENS-401), an orally active calcineurin inhibitor, has been demonstrated to mitigate cisplatin-induced hearing loss and cochlear damage [1][2].

Amifostine trihydrate (WR2721) is the first approved radioprotective drug, used to decrease the risk of kidney problems caused by treatment with cisplatin.

PHD2 HDACs-IN-1 is a potent mixed inhibitor of PHD2 HDACs, acting on PHD2 (IC50: 1.15 μM), HDAC1 (IC50: 19.75 μM), HDAC2 (IC50: 26.60 μM), and HDAC16 (IC50: 15.98 μM). HDACs-IN-1 is a low toxicity nephroprotective agent suitable for studies of cisplatin-induced acute kidney injury (AKI).

Ansatrienin B is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis., In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 21 nM), which is a measure of bone resorption, and pp60c-src kinase (IC50 = 50 nM). It is an inhibitor of translation at the protein synthesis stage by specific inhibition of L-leucine incorporation (IC50 = 58 nM in A549 cells). It also inhibits TNF-α-induced expression of intercellular adhesion molecule-1 (ICAM-1; IC50 = 300 nM). Early in vitro studies showed that ansatrienin B potentiates the chemotherapeutic action of 5-fluorouracil , cisplatin , bleomycin , mitomycin C , and 6-mercaptopurine. Ansatrienin B is a hydroquinone form of ansatrienin A .

E-3620 is a novel 5-HT3 receptor antagonist that inhibits cisplatin-induced vomiting in beagles. E-3620 can be used to study dyskinesia, gastrointestinal dyskinesia, psoriasis and psoriasis.

AKR1B10-IN-1, a powerful AKR1B10 (Aldo-Keto Reductase 1B10) inhibitor, demonstrates an IC50 value of 3.5 nM. This compound effectively curtails the proliferation, metastasis, and Cisplatin (CDDP) resistance of lung cancer cells.

KX1-141 is an Src-protein tyrosine kinase inhibitor, which may reduce cisplatin ototoxicity while preserving its antitumor effect.

1. Ganoderic acid A exhibits antitumor activity, mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1. 2. Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human

LLL12, a small molecule inhibitor of STAT3, inhibits STAT3 phosphorylation and enhances the inhibitory effects of Cisplatin and Paclitaxel on ovarian cancer cell formation, migration, and growth [1].

Phenanthriplatin, also known as cis-[Pt(NH3)2-(phenanthridine)Cl]NO3, is a new drug candidate. It belongs to a family of platinum(II)-based agents which includes cisplatin, oxaliplatin and carboplatin. Phenanthriplatin Acts As a Covalent Poison of Topoiso

ERCC1-XPF-IN-2 is active in nucleotide excision repair, cisplatin enhancement and γH2AX assays. ERCC1-XPF-IN-2 is a potent inhibitor of ERCC1-XPF endonuclease with an IC 50 value of 0.6 μM [1].

NHEJ Inhibitor-1 (Compound C2), a trifunctional Pt(II) complex, mitigates non-homologous end joining (NHEJ)/homologous recombination (HR)-related double strand break (DSB) repairs, combating Cisplatin resistance in non-small cell lung cancer (NSCLC). It achieves this by inhibiting the damage repair proteins Ku70 and Rad51, thus re-sensitizing tumors to Cisplatin. Additionally, this compound prompts the generation of reactive oxygen species (ROS) and reduces mitochondrial membrane potential (MMP) [1].

NecroIr1, an iridium(III) complex, acts as a necroptosis inducer in Cisplatin-resistant lung cancer cells (A549R). It selectively targets mitochondria, causing oxidative stress and reducing mitochondrial membrane potential (MMP). By activating receptor-interacting serine-threonine kinase 3 (RIPK3) and Mixed Lineage Kinase (MLKL), and modulating CDK4 expression, NecroIr1 facilitates cell death mechanisms [1].

84-B10, a derivative of 3-phenylglutaric acid, inhibits cisplatin-induced tubular ferroptosis, attenuates mitochondrial damage and oxidative stress, and ameliorates acute kidney injury (AKI) resulting from cisplatin administration [1].

Lactate Transporter 1 (Compound 1) serves as an active lactate transporter within living cells and exerts cytotoxic effects, exhibiting IC50 values of 3.36 μM in HeLa, 3.27 μM in CAL27, 5.58 μM in MCF7, and 7.66 μM in MCF10A cells. Additionally, an additive effect with Cisplatin has been observed in HeLa cells [1].

Sageone represents a promising anticancer agent against gastric cancer that warrants further study, it synergizes with cisplatin cytotoxicity in SNU-1 human gastric cancer cells.Sageone also shows antiviral activity.

Isodonal shows abilities to inhibit K562 cells camparable to that of cisplatin.

Indium (III) thiosemicarbazone 5b is an anticancer compound demonstrating cytotoxicity against various cancer cell lines including A549, MCF-7 breast, cisplatin-resistant MCF-7/DDP breast, and Hl 7702 liver cancer cells, with IC50 values of 2.41, 1.97, 2.11, and 8.95 µM, respectively. It effectively lowers PI3K, Akt, mTOR, P-gp, and GSH levels in MCF-7/DDP cells. In vivo studies show that at a dosage of 2.5 µmol/kg, indium (III) thiosemicarbazone 5b significantly reduces tumor weight and volume in MCF-7/DDP mouse xenograft models. Furthermore, liposomes formulated with this compound promote apoptosis and pro-death autophagy in MCF-7/DDP cells, alongside notable reductions in tumor volume and weight, showcasing its potential as a therapeutic agent in cancer treatment.

LC28 is a novel inhibitor of STAT3 signaling, suppressing survival of cisplatin-resistant ovarian cancer cells.

Iproplatin is a synthetic second-generation platinum-containing compound related to cisplatin. Iproplatin binds to and forms DNA crosslinks and platinum-DNA adducts, resulting in DNA replication failure and cell death. Although less prone to glutathione i

ROS-ERS inducer 1, a type II immunogenic cell death (ICD) inducer, is a Pt(II)-N-heterocyclic carbene (Pt(II)-NHC) complex derived from 4,5-diarylimidazole. It induces endoplasmic reticulum stress (ERS) along with reactive oxygen species (ROS) generation, leading to the release of damage-associated molecular patterns (DAMPs) in HCC cells, showcasing significantly higher anticancer activities than Cisplatin [1].

Riviciclib hydrochloride (P276-00) is a novel inhibitor of CDK1, CDK4, and CDK9, with IC50 values of 79 nM, 63 nM, and 20 nM, respectively, currently in Phase 2 3.

Monoolein (1-Oleoyl-rac-glycerol) is a surfactant that releases free glycerol and oleic acid upon hydrolysis. Monoolein has been used in liquid crystal studies and research shows that in the presence of monoolein, the penetration of the drug cisplatin (sc-200896) is doubled.

Heptaplatin, a new platinum derivative with anticancer activity, is used against various cancer cell lines, including cisplatin-resistant cancer cell lines. It has been reported to have a response rate of 17% as a single agent, and tolerable toxicity in t

RIPK3-IN-4 (Compound 42) is a RIPK3 inhibitor that mitigates necroptosis, inflammatory responses, and HK-2 cell damage. It alleviates acute kidney injury by attenuating Cisplatin- and I R-induced kidney damage, along with associated inflammatory responses and necroptosis [1].

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

(rel)-Oxaliplatin, a DNA synthesis inhibitor, induces DNA crosslinking damage, inhibits DNA replication and transcription, and stimulates apoptosis. This compound has applications in cancer research [1] [2] [3].