Ciclo celular / Checkpoint

<p>PD-1/PD-L1-IN-27: potent anti-cancer, IC50 134nM, minimal T cell harm, boosts CD8+ T cells, reduces fatigue.</p>

<p>USP1-IN-5 (compound 10) is a potent inhibitor of both USP1, with an IC50 of less than 50 nM, and MDA-MB-436 cells, where it also exhibits an IC50 of less than</p>

<p>Cdc7-IN-7 is a potent inhibitor of Cdc7 kinase.</p>

<p>8-Azahypoxanthine (NSC-22709) inhibits hypoxanthine-guanine-xanthine phosphoribosyltransferase and has antimalarial properties.</p>

<p>Aurora kinase inhibitor-8 is a highly selective inhibitor of Aurora kinase.</p>

<p>Inixaciclib is a potent CDK inhibitor, can be used to research anticancer.</p>

<p>Halofuginone hydrochloride (RU-19110), a derivative of Febrifugine, functions as a competitive inhibitor of prolyl-tRNA synthetase, displaying a Ki value of 18.3 nM. This compound effectively inhibits type-I collagen synthesis, providing therapeutic benefits in osteoarthritis (OA) by impeding TGF-β signaling. Additionally, it serves as a potent pulmonary vasodilator, mainly through the activation of Kv channels and the inhibition of various calcium channels including voltage-gated, receptor-operated, and store-operated ones. Beyond its vascular effects, Halofuginone hydrochloride exhibits a broad spectrum of biological activities, including anti-malarial, anti-inflammatory, anti-cancer, and anti-fibrotic properties, supported by multiple studies.</p>

<p>CI 972 anhydrous is an inhibitor of purine nucleoside phosphorylase (PNP) (Ki: 0.83 μM) used as a T cell-selective immunosuppressive agent.</p>

<p>PLK4-IN-4 (compound 22), a potent inhibitor of PLK4, exhibits an IC50 value of 7.9 nM, suggesting its potential use in cancer research [1].</p>

<p>TC-A 2317 HCl inhibits Aurora A kinase (Ki 1.2 nM) over Aurora B (Ki 101 nM), displaying antitumor effects.</p>

<p>NTRC 0066-0 is a TTK inhibitor that can be used in cancer research.</p>

<p>Tirofiban HCl is an antagonist of platelet glycoprotein-IIb/IIIa receptor.</p>

<p>NU6300 is a covalent CDK2 inhibitor exhibiting irreversible and ATP-competitive properties and also functions as a GSDMD (Gasdermin D) inhibitor.</p>

ML-099 is a pan Ras-related GTPases activator that activates Rac1, Ras, GTP-binding protein (Rab7), Rab2A and cell division cycle 42.

<p>SZ-015268: CDK7 inhibitor, IC50=23.56 nM; hinders HCC70, OVCAR-3, HCT116, HCC1806 cell growth; strong anti-tumor effect.</p>

<p>8-NH2-ATP tetrasodium, an inactive ATP variant, originates from 8-NH2-Ado tetrasodium, which triggers the apoptosis-associated cleavage of poly (ADP-ribose) polymerase [1] [2].</p>

<p>SC-52012 is a novel and potent fibrinogen receptor antagonist, an RGD mimetic, which inhibits platelet aggregation.</p>

<p>CDK4/6-IN-15: Oral, selective CDK4/6 inhibitor, halts cancer cell growth, G1 arrest, suppresses Rb phosphorylation.</p>

<p>KY386 is a potent and selective DHX33 helicase inhibitor with an IC50 value of 19 nM.</p>

<p>UNC-2170 (UNC2170 Maleate) is the methyl-lysine binding protein, 53BP1 ligand.</p>

<p>BI-1950: potent inhibitor of LFA-1, key in immune function and drug target.</p>

<p>BMT-090605: AAK1 inhibitor (IC50=0.6 nM), also affects BIKE (45 nM) and GAK (60 nM), has antinociceptive properties.</p>

<p>VER-00158411 is a checkpoint kinase 1 and CHK2 inhibitor (IC50: 4.4 nM and 4.5 nM, respectively).</p>

<p>Myt1-IN-3 is a potent inhibitor of Myt1 (IC50 &lt;10 nM) [1].</p>

<p>Fosfluridine tidoxil, a thymidylate synthase inhibitor, is used potentially for the treatment of colorectal cancer, and breast cancer.</p>

<p>L-Methioninamide hydrochloride is a potent inhibitor of methionyl-tRNA synthetase that reduces the toxicity of CDDP.</p>

<p>Mevociclib (SY-1365) is a highly selective covalent inhibitor of CDK7. SY-1365 possesses therapeutic potential in both hematological and solid tumors.</p>

<p>PDD00031705 is a benzimidazolone core cell-inactive Poly (ADP-ribose) glycohydrolase (PARG) inhibitor.</p>

<p>Palmitoyl 3-carbacyclic phosphatidic acid, a palmitoylated Carba-like cyclophosphatidic acid and LPA (lysophosphatidic acid) analog, possesses distinct biological activities compared to LPA, including the inhibition of RhoA activation and melanoma cell migration. This compound has demonstrated efficacy in inhibiting experimental lung metastasis and reducing tumor nodule counts in a B16-F0 xenograft mouse model [1].</p>

<p>Cdc7-IN-12, a sub-1 nM CDC7 inhibitor, may aid cancer research; hinders COLO205 cell growth (IC50: 100-1000 nM).</p>

<p>Xylocydine is a novel Cdk inhibitor that induces apoptosis in HCC, suppresses tumor growth, and is non-toxic to other tissues.</p>

<p>DCB-3503, a tylophorine analog, may fight cancer and aid immunosuppression by hindering protein synthesis and modulating HSC70 ATPase function.</p>

<p>Pen is an oral cancer drug that blocks DNA synthesis by inhibiting key enzymes and integrating into DNA.</p>

<p>Wee1 Inhibitor I is an ATP-binding site-targeting Wee1 inhibitor.</p>

<p>Trovafloxacin: broad-spectrum fluoroquinolone, blocks DNA gyrase/topoisomerase IV and PANX1 channel (IC50=4μM).</p>

<p>Litronesib is a selective inhibitor of mitosis-specific kinesin Eg5. It also has antitumor activity.</p>

<p>RAD51-IN-4, a potent RAD51 inhibitor, may be useful in researching mitochondrial defect-related conditions.</p>

<p>Myt1-IN-2, a highly potent Myt1 inhibitor, exhibits remarkable anticancer properties with an IC50 value below 10 nM (WO2021195782A1; compound 28) [1].</p>

<p>ICAM-1-IN-1 is a potent and selective E-selectin(IC50 = 7 nM) and ICAM-1(IC50 = 5 nM) inhibitor.</p>

<p>L 738167 is a potent antagonist of the long-acting fibrinogen receptor.</p>

<p>LX7101 is a potent inhibitor of both LIM kinase (LIMK) 1 and 2, and Rho-associated kinase 1 (ROCK1) and ROCK2, with IC50 values of 32, 4.3, 69, and 32 nM, respectively. It is selective, demonstrated by its lack of cross-reactivity in a panel of binding assays involving 78 receptors, transporters, and an additional 430 kinases, at a concentration of 10 μM. The topical administration of LX7101 (3 μl of a 1 mg/ml solution) to the eye has been shown to reduce intraocular pressure in a dexamethasone-induced mouse model of glaucoma.</p>

<p>CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).</p>

<p>Voruciclib hydrochloride is an orally active and selective inhibitor of CDK (Ki: 0.626 nM-9.1 nM).</p>

<p>Alatrofloxacin is a prodrug of trovafloxacin.</p>

<p>ROCK2 inhibitor is a chemical compound associated with the therapeutic management of psoriasis.</p>

<p>NITD008 (7-Deaza-2'-C-acetylene-adenosine) is an adenosine nucleoside inhibitor with antiviral activity that inhibits dengue and Zika viruses.</p>

<p>G4/HDAC-IN-1, a G4/HDAC dual inhibitor, IC50 1.1 µM, blocks TNBC growth, useful in cancer research.</p>

Debio-0123: potent, specific oral WEE1 inhibitor; IC50 in low nanomolar; boosts DNA damage & Carboplatin's anti-cancer effects.

<p>CFI-402257 is a selective inhibitor of Mps1/TTK kinase (Mps1 Ki = 0.09 nM; EC50 = 6.5 nM)and can be used in studies about hepatocellular carcinoma diseases.</p>

<p>Thymectacin (NB 1011) is a selective thymidine synthase (TS) inhibitor with anticancer activity for the study of colon cancer and solid tumors.</p>