T2066

Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.

Revaprazan is a novel, selective potassium-competitive acid blocker, to be specific, it reversibly inhibits gastric H(+)/K(+)-ATPase and shows effective acid suppression comparable to PPIs.

(S, R, S)-AHPC-PEG4-tosyl is a PROTAC linker that connects an E3 ligase ligand with a PEG4 linker, facilitating PROTAC drug research and discovery. The PEG4 spacer increases the hydrophilicity of the compound. The tosyl group reacts with amines or other nucleophiles.

KU13 is an inhibitor of non-tuberculous mycobacteria (NTM), demonstrating minimum inhibitory concentrations (MIC) of 0.032-8 μg/mL against Mycobacterium and 2 μg/mL against E. coli. It is applicable in research focused on anti-infective treatments.

Tulobuterol is mainly used for the prevention and treatment of bronchial asthma, asthmatic bronchitis and chronic bronchitis. Research shows that it could inhibit rhinovirus infection in primary cultures of human tracheal epithelial cells.

Enozertinib is an EGFR inhibitor with antitumor properties.

Florfenicol-propanoate-piperidin (Compound 1) is a derivative of Florfenicol. This compound exhibits antibacterial activity, effectively inhibiting strains such as E. coli ATCC25922, Salmonella CICC110420, S. aureus ATCC29213, B. subtilis CMCC(B)63501, E. faecalis ATCC29212, S. suis CVCC606, and Haemophilus parasuis, with a minimum inhibitory concentration (MIC) ranging from 2 to 8 μM.

CDD-2789 is a highly selective small molecule inhibitor that targets Activin receptor type 1 (ALK2, also known as ACVR1). It effectively blocks the BMP and activin A-induced downstream phosphorylation reactions by inhibiting the ALK2/ALK1-mediated SMAD1/5 signaling pathway. In the NanoBRET cell model, CDD-2789 demonstrates an inhibitory activity with an IC50 value of 0.54 µM for ALK2. This compound holds potential for research in ALK2-related diseases, including brainstem glioma (DIPG), ependymoma, endometrial cancer, melanoma, non-small cell lung cancer, colorectal cancer, and pancreatic cancer.

Gemifloxacin is a fluoronaphthyridone with strong antibacterial effect.

Ethanol-D6 is the deuterium-labeled form of ethanol.

HDAC-IN-27 dihydrochloride (Compound 11h) is a potent, orally active, HDACI class-selective inhibitor, with IC50 values ranging from 0.43 to 3.01 nM for HDAC1-3. This compound exhibits both in vivo and in vitro anticancer activity. HDAC-IN-27 shows significant antiproliferative effects against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). It is useful for research on acute myeloid leukemia (AML).

TNF-α-IN-22 (Compound 30) is a TNFα inhibitor that induces apoptosis by inhibiting TNFα-induced IkBα downregulation and blocking the cell cycle. It is applicable for research in triple-negative breast cancer.

8-Oxo-dATP can be hydrolyzed to its monophosphate form by the oxidation of purine nucleoside triphosphate MTH1, preventing erroneous incorporation during DNA replication or transcription.

(1R,2S,3R)-Aprepitant (Compound ent-4) is a competitive antagonist of the human neurokinin-1 (NK-1) receptor. It holds potential for research in the treatment of nausea and vomiting related to cancer or postoperative conditions.

SIK2/3-IN-1 (Compound 7S) is an orally active and selective inhibitor of SIK2/3. It significantly inhibits tumor growth without causing weight loss in the MV4-11 AML mouse CDX model. SIK2/3-IN-1 is applicable for research in MEF2C-dependent acute myeloid leukemia.

(S)-PI3K-IN-2 is the enantiomer of PI3K-IN-2, functioning as a ΡΙ3Κβ/δ inhibitor with IC50 values of 0.198 and 0.282 μM, respectively. It can also inhibit the phosphorylation of AKT(ser473) in MDA-MB-468 cells, with an IC50 of 27 nM.

MAGLLigand-Linker Conjugate 1 is a compound that combines a MAGL ligand with a linker. This conjugate serves as an essential component for synthesizing the PROTAC degrader, known as PROTACMAGLdegrader-1.

MSRV-IN-1 (Compound M3) is an inhibitor targeting aquatic rhabdoviruses, including MSRV, SVCV, and IHNV, with IC50 values of 0.92 μM, 2.92 μM, and 2.78 μM, respectively. Instead of acting directly on virus particles, MSRV-IN-1 disrupts the replication environment by altering the virus-induced S-phase cell cycle arrest, inhibiting viral replication. Administered via intraperitoneal injection at a dose of 20 mg/kg, MSRV-IN-1 significantly improves the survival rate of MSRV-infected largemouth bass by 35.98% and reduces viral load in the liver, spleen, and kidneys. MSRV-IN-1 is applicable in research on rhabdovirus-associated diseases in aquaculture.

Ran-IN-1 (Compound M36) is an orally active and selective inhibitor of Ran GTPase. It binds allosterically with high specificity to the switch II pocket of GDP-bound Ran (RanGDP), stabilizing its inactive state and reducing the formation of active Ran-GTP. Ran-IN-1 induces apoptosis in epithelial ovarian cancer (EOC) cells and inhibits DNA repair pathways such as homologous recombination (HR) and non-homologous end joining (NHEJ). This compound shows potential for research in epithelial ovarian cancer, particularly in high-grade serous carcinoma.

Antitumor agent-202 is a stabilizer of the p53Y220C mutant, selectively inhibiting the proliferation of tumor cells carrying the p53Y220C mutation. It is applicable for research focused on cancers associated with the p53 Y220C mutation.

Racemic Naproxen is a biochemical substance.

5-APDI hydrochloride is an indane featuring an amphetamine-like aminopropyl group. It acts as an inhibitor of serotonin, dopamine, and norepinephrine uptake by synaptosomes, with IC50 values of 82 nM, 1,847 nM, and 849 nM, respectively.

LPA2 antagonist 5 (EX1) functions as an antagonist of LPA2, with an IC50 value of 4.05 nM.

TYK2ligand 2 is the TYK2 ligand of PROTACTYD-68. TYD-68 is a highly potent and selective CRBN-recruiting TYK2 PROTAC degrader with a DC50 value of 0.42 nM.