is-145

IS-145 is a thromboxane A2 receptor antagonist.

QQN-00358 is a novel potent and selective tankyrase (TNKS) inhibitor.

CDK9-IN-7 is a highly selective and orally active CDK9/cyclin T inhibitor (IC50: 11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD: 148 nM; CDK6/cyclinD: 145 nM).

MSC2360844 is a potent, orally active and selective inhibitor of PI3Kδ(IC50 of 145 nM).

Duvelisib (INK1197, IPI-145) is a selective inhibitor of phosphatidylinositol 3-kinase (PI3K) and p100δ, with effects on p110δ (IC50 value is 0.0025 μM), p110γ (IC50 value is 0.274 μM), p110β (IC50 value is 0.85 μM) and p110α (IC50 value is 1.602 μM).

Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx.

Lidocaine hydrochloride (Lignocaine hydrochloride) is a local anesthetic and cardiac depressant used as an antiarrhythmic agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.

Duvelisib R enantiomer (IPI-145 R enantiomer) is an enantiomer of Duvelisib with lower activity. Duvelisib is a PI3K inhibitor.

FAAH-IN-1 is a fatty acid amide hydrolase (FAAH) inhibitor with IC50 values of 145 nM for rat FAAH and 650 nM for human FAAH.

ML 145 is a selective and potent antagonist of human GPR35, with no significant activity against GPR35 in any of its immediate rodent homologs.ML 145 has potential anti-inflammatory activity for the study of immunoinflammation.ML 145 is a novel non-steroidal anti-inflammatory agent for the study of rheumatoid arthritis.

Mps1-IN-2 is a potent, selective, and ATP-competitive inhibitor of both Mps1 and Plk1.

GSTP1-1 inhibitor 2 (Compound 5g) is an inhibitor of hGSTP1-1 (glutathione S-transferase P1-1), exhibiting an IC50 of 12.2 μM. It demonstrates substantial cytotoxicity against the cell lines DU-145, PC3, and MCF-7, with CC50 values of 36.6, 11.9, and 17.4 μM respectively, making it relevant for research in cancer therapeutics.

E3 Ligase Ligand-linker Conjugate 145 is a combination of an E3 ubiquitin ligase ligand and a linker, utilized in the synthesis of PROTACAR Degrader-7.

Aurora A inhibitor4 (compound C9) is a potent inhibitor of Aurora A, with GI50 values of 4.26 μM in DU 145 cells and 7.08 μM in HT-29 cells.

EGFR-IN-145 (compound 7c) is an EGFR kinase inhibitor. At a concentration of 20 μM, it inhibits wild-type EGFR kinase by 52.7%.

Anticanceragent 264 (Compound 5w) is an anticancer compound that exhibits significant antiproliferative activity in tumor cell lines, with an IC50 range of 7.5-33.67 μM. It notably induces cell cycle arrest at the G2/M phase in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines. This compound reduces key cell cycle proteins CDK1, CDK2, and Cyclin B1 in a dose-dependent manner and has strong binding activity with differentiation inhibitors and DNA-binding proteins. Anticanceragent 264 is useful for research in the cancer disease domain.

CYP17A1-IN-1 (Compound 14) is an inhibitor of CYP17A1 with an IC50 of 26 nM. It exhibits cytotoxicity in androgen-sensitive prostate cancer cells, specifically LNCaP, and hinders the migration of DU-145 cells.

PLK1-IN-14 (Compound Hit-4) is a selective PLK1 inhibitor with an IC50 of 22.61 pM for PLK1, and an IC50 of 0.09 nM for inhibiting the proliferation of DU-145 prostate cancer cells. It is applicable in prostate cancer research.

GLI1-IN-3 (Compound 11a) is a triterpenoid-like compound that inhibits Hedgehog signaling in cancer cells with GLI1 overexpression. It suppresses the proliferation of non-small cell lung cancer and prostate cancer cell lines with excessive Hh signaling activation. Additionally, GLI1-IN-3 reduces the expression of GLI1 protein and its target genes associated with tumor progression and proliferation in A549 and DU-145 cancer cells.

CDK2-IN-45 is a CDK2 inhibitor with an IC50 value of 0.64 μM. It effectively inhibits the proliferation of DU-145 and PC-3 cell lines, with IC50 values of 2.20 μM and 4.17 μM, respectively. Additionally, CDK2-IN-45 induces G0/G1 phase cell cycle arrest and apoptosis. It is utilized in prostate cancer research.

ADAR1-IN-1 is a potent ADAR1 inhibitor. It significantly suppresses the proliferation of DU-145 cells (IC50 = 1.11 μM), inhibits colony formation, migration, and invasion, and induces cell cycle arrest and apoptosis. ADAR1-IN-1 effectively and safely impedes tumor growth and can be utilized in prostate cancer (PCa) research.

MSC778 is a selective and orally active inhibitor of flap endonuclease 1 (FEN1), with an IC50 of 3 nM and a KD of 2.9 nM. It exhibits 145-fold, 516-fold, and 65-fold selectivity over EXO1, GEN1, and XPG, respectively. MSC778 selectively targets BRCA2-deficient cells and enhances the tumor-stalling activity of Niraparib in BRCA2 KO DLD-1 mouse xenografts. It is applicable in colorectal cancer research.

HDAC6-IN-63 (Compound 7) is an orally active inhibitor of HDAC6 with an IC50 of 145 nM. It suppresses the expression of Sp1 and RAD51, inducing caspase-dependent apoptosis. HDAC6-IN-63 exhibits antitumor activity and enhances the sensitivity of Etoposide and Gemcitabine by inhibiting homologous recombination and non-homologous end joining (NHEJ) pathways involved in DNA double-strand break (DSB) repair, promoting synergistic cell death in NSCLC cells. This compound is applicable for chemotherapy research in cancers such as NSCLC.

Antifungalagent 145 (Compound 14') is a potent antifungal agent. It exhibits minimum inhibitory concentrations (MICs) of 4, 8, and 8 μg/mL against Candida albicans, Candida tropicalis, and Cryptococcus neoformans, respectively. By disrupting fungal cell membranes, Antifungalagent 145 rapidly eradicates fungi and effectively inhibits and degrades biofilms. It offers improved safety for use in antifungal research.