Trimelamol (CB10-375; NSC283162) is a highly efficient acid-catalyzed DNA interstrand crosslinker with low neurotoxicity due to its limited BBB penetration. Trimelamol exhibits anti-tumor activity and overcomes platinum resistance. Trimelamol is investigated for lung and ovarian cancer research[1][2][3][4][5].

YTK-1305 is a p62 ligand compound that promotes cellular autophagy.

DBM-819 is a reversible inhibitor of H⁺/K⁺-ATPase (H+/K+-ATPase), with an IC50 value of 5 μM. DBM-819 can reversibly block gastric acid secretion by inhibiting the proton pump in the gastric mucosa. It shows significant protective effects against duodenal ulcers induced by Cysteamine, gastric ulcers induced by Indomethacin, and gastric ulcers induced by Aspirin, with EC50 values of 6, 3.1, and 4 mg/kg respectively. DBM-819 can be used in ulcer prevention research.

BJH-60 is a mitochondrial complex 1 inhibitor. BJH-60 can inhibit mitochondrial oxygen consumption rate with an IC50 of 1.9 μM in A549 cells. BJH-60 shows no PDE inhibitory effect. BJH-60 can be used for the research of cancer, such as breast cancer.

KI-TOX-A3 is a selective protein-protein interaction (PPI) inhibitor targeting TOX protein (with an IC50 value of 0.51 μM for TOX-KAT7 interaction). KI-TOX-A3 induces proteasomal degradation of TOX, restores KAT7-mediated H3K14 acetylation, reversing CD8+ T cell exhaustion and inhibiting T-cell acute lymphoblastic leukemia (T-ALL) cell proliferation. KI-TOX-A3 is promising for research of hematological tumors (e.g., T-ALL).

PAB-(PEG4-Me)-Cit-Val-PEG2-amide-C2-MC is an ADC linker that can be combined with the TLR7/8 agonist for the synthesis of a linker-payload conjugate.

pro-FTY, a FTY720 anticancer prodrug, is a sphingosine-1-phosphate (S1P) inhibitor. pro-FTY specifically inhibits S1P signaling in cancer cells using a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly inhibits the survival of breast cancer cells, including multidrug-resistant cells and its organoids resistant to Paclitaxel or Doxorubicin. pro-FTY potently suppresses tumor growth in 4T1 cells or organoids xenograft tumors mice model while avoiding lymphocytopenia.

(R)-thioxo-Dxd is a Camptothecin derivative. (R)-thioxo-Dxd can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. (R)-thioxo-Dxd can be used for research on tumors with high HER2 or TROP2 expression.

thioxo-Dxd is a Camptothecin derivative. thioxo-Dxd can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. thioxo-Dxd can be used for research on tumors with high HER2 or TROP2 expression.

KW-2450 tosylate is an orally active Aurora A and B kinases, IGF-1R, and IR tyrosine kinases inhibitor. KW-2450 tosylate induces Apoptosis. KW-2450 tosylate also exhibits anticancer activity against triple-negative breast cancer.

502U83 is an anti-cancer agent. 502U83 can inhibit DNA and RNA synthesis (IC50 ≈ 30 µM). 502U83 can be used for research on cancers such as leukemia.

(2R,4R,6S)-Tubacin is the 2R,4R,6S enantiomer of Tubacin. Tubacin is a potent and selective inhibitor of HDAC6, with an IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1. Tubacin also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).

ESP-31015 (ETC-1001) is an orally active and non-fibrate based PPARα agonists. ESP-31015 demonstrates significant lipid-regulating effects in the obese Zucker rat model. ESP-31015 can be used in cardiovascular disease research.

Psicose is a natural and low-calorie sweetener. Psicose can activate the PI3K/Akt/mTOR pathway to promote muscle synthesis. Psicose can upregulate IGF-1 and downregulate Myostatin. Psicose regulates mitochondrial function by increasing G6P activity. Psicose enhances antioxidant enzyme activity and reduces oxidative stress markers. Psicose reduces plasma triglycerides and total cholesterol. Psicose can improve muscle fiber size and reduce fibrosis. Psicose can be used for research on sarcopenia.

PVTX-321 (Compound 16a) is an orally active estrogen receptor α (ERα) degrader. PVTX-321 can potently degrade ERα (DC50=0.15 nM in MCF-7 cells) and also has inhibitory activity against mutant ERα (IC50=59 nM). PVTX-321 is promising for research of ER+/HER2- breast cancer.

RU-24213 hydrochloride is a selective D-2 dopamine receptor agonist. RU-24213 hydrochloride is also a KAPPA-opioid receptor antagonist. RU-24213 hydrochloride induces stereotyped behaviors.

7-Hydroxy-DPAT (7-OH-DPAT) is a selective D3 dopamine receptor agonist. 7-Hydroxy-DPAT exhibits significant pharmacological activity in modulating locomotor behavior and dopamine metabolism within the brain. 7-Hydroxy-DPAT can be used for the research of neurological disease .

RK-851 is a highly selective and orally active δ-opioid receptor antagonist, with a negative logarithm of the antagonist concentration (pA2) of 8.84. TRK-851 exhibits the selectivity for the δ receptor of more than 100 times higher than that for the μ or κ receptors. TRK-851 exhibits a potent antitussive effect in a rat model of capsaicin-induced cough. TRK-851 can be used for research on antitussive effects.

2-Fluorodeoxyarbutin, a derivative of Deoxyarbutin, is a tyrosine hydroxylase and dopa oxidase inhibitor. 2-Fluorodeoxyarbutin inhibits melanin synthesis in intact melanocytes. 2-Fluorodeoxyarbutin can be used for the strudy of skin lightening or for ameliorating hyperpigmented lesions.

SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. SMU-R39 binds to recombinant mTLR7 protein (KD = 2.36 μM) and to recombinant hTLR8 protein (KD = 105 nM). SMU-R39 suppresses downstream NF-κB and MAPK signaling, and reduces secretion/transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. SMU-R39 demonstrates anti-inflammatory efficacy in Imiquimod (IMQ)-induced psoriasis mouse model. SMU-R39 can be used for the study of autoimmune diseases such as psoriasis.

NO-Rosa5 (chloride) is a photocontrollable NO donor. NO-Rosa5 (chloride) is made up of the fluorescent dye rosamie that functions as the light-harvesting group.

Papaveroline is a Fyn Tyrosine Kinase inhibitor. Papaveroline can be used for the research of neurological disease, such as Alzheimer's disease (AD).

ML-20, Malabaricone C analogue, is a autophagy inhibitor and radiosensitizer. ML-20 inhibits cell growth, induces cell apoptosis . ML-20 induces DNA double-strand breaks, loss of mitochondrial membrane potential (MMP), and lysosomal membrane permeabilization (LMP). ML-20 induces endoplasmic reticulum stress and concurrent inhibition of autophagy flux due to LMP .

SB-583355 (Compound 56) is a potent G2A antagonist. SB-583355 can be prepared by a Suzuki reaction between 4-methoxyphenyl boronic acid and 3-bromo-4-hydroxybenzoic acid following the conditions followed by an amide coupling reaction. SB-583355 blocks the activation of G2A mediated either by 9-HOPE or T-10148 in human G2A expressing CHO-K1 cells. SB-583355 can be studied in research for inflammation, myeloid leukemia, and neuropathic pain.

Vilanterol (GW642444) acetate is a long-acting β2 adrenergic receptor agonist. Vilanterol acetate has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research[1][2].

LM-189, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 can be used to develop the Gαi-biased β2AR agonists.

LM-189 free base, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 free base stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 free base can be used to develop the Gαi-biased β2AR agonists.

RD0392 (Compound 5) is a competitive tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC50=1.3 nM). RD0392 is promising for research of neurodegenerative diseases like Alzheimer’s.

Salvianolic acid A derivative-1 (Compound SAA-30) is a orally active derivative of Salvianolic acid A. Salvianolic acid A derivative-1 binds to transgelin with a KD of 2.39 μM. Salvianolic acid A derivative-1 promotes cell contractions by facilitating the aggregation of actin. Salvianolic acid A derivative-1 can be used for prevention of myocardial ischemia or other diseases associated with IR tissue injuries.

HEAL-116 is a potent, specific and orally active 3β-hydroxysteroid dehydrogenase type 1 (3βHSD1) inhibitor with an IC50 of 1.18 μM and a KD of 1.32 μM. HEAL-116 inhibits DHEA metabolism and DHEA-induced target gene expression and cell proliferation. HEAL-116 can be used for cancer research, such as prostate cancer.