phenotype

Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive, and orally active pan-PTP (protein tyrosine phosphatases) inhibitor with insulin-mimicking effects and anti-diabetic properties. BMOV is a potent insulin sensitizer and has been shown to improve cardiac dysfunctions in diabetic models. BMOV inhibits HCPTPA, PTP1B, HPTPβ, and SHP2 with IC50s of 126 nM, 109 nM, 26 nM, and 201 nM, respectively [1][2].

NKL 22 (Histone Deacetylase Inhibitor IV) is an effective Histone Deacetylase Inhibitor.

GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fol

BML-284 (Wnt agonist 1) is a potent, selective and , cell-permeable Wnt signaling activator.

Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.

BML-284 hydrochloride (Wnt agonist 1 HCL) is a potent, selective Wnt canonical signaling activator and tubulin polymerization inhibitor.

Haptoglobin, Phenotype 2-2 is a plasma protein that binds hemoglobin (Hb) to remove free hemoglobin and possesses antioxidant activity. It can be utilized in research related to kidney failure and cardiovascular diseases associated with diabetes.

Hepln-13 is a hepsin inhibitor that acts by hindering prostate cancer bone metastasis.

DZ2002, an orally active, reversible, and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), exhibits significant immunosuppressive activity. It effectively prevents experimental dermal fibrosis by reversing the profibrotic phenotype in multiple cell types, making it useful for studying autoimmune diseases like lupus syndrome and systemic sclerosis.

AZD-4877 is a potent spindle kinesin (Eg5) inhibitor with an IC50 value of 2 nM. AZD-4877 is an alternative configuration of Ispinesib that inhibits mitosis, induces the formation of a unipolar spindle phenotype, and mediates apoptosis. AZD-4877 has antitumor activity and inhibits circulating peripheral blood mononuclear cells (PBMC).

NSC-16590 (2-Aminoisobutyric acid) is a nonprotein amino acid (is an end product of pyrimidine Metabolism) excreted in the urine of about 5% of healthy individuals, and high excretion is an autosomal recessive phenotype.

Butyrolactone II (A9) exhibits DPPH radical scavenging activity with an EC50 value of 42.05 μM, superior to the positive control BHT. Butyrolactone II (A9) demonstrates neuroprotective activity in Caenorhabditis elegans CL2355 by alleviating Aβ-induced chemotaxis disorder, prolonging lifespan, and reducing 5-HT sensitivity, and is utilized in neurodegeneration research focused on oxidative stress mitigation, amyloid-associated functional impairment, and behavioral phenotype modulation in nematode models.

GTCpFE, a compound synthesized from Dimethyl fumarate (DMF) and Aspirin (ASA), inhibits IKKα/β in the NF-κB pathway, exhibiting anti-inflammatory activity by preventing p65 from entering the nucleus. It selectively inhibits cancer stem cell (CSC) activity by reducing the growth of mammospheres and the expression of the CD44+CD24- immune phenotype. Furthermore, GTCpFE targets breast cancer stem cells, crucial in aggressive cancer phenotypes that depend on NFκB and PGE2.

TB22 is a non-nucleoside inhibitor of DOT1LR231Q with anticancer activity. It inhibits the malignant phenotype of lung cancer cells harboring the R231Q mutation via the MAPK/ERK signaling pathway, making it useful for lung cancer research.

Neuroprotective agent 5 (compound 28) acts as a brain-penetrating agent with anti-neuroinflammatory, antioxidant, and neuroprotective properties. It exhibits potent inhibition of nitric oxide (NO) with an EC50 of 0.49 μM and suppresses the release of pro-inflammatory mediators PGE2 and TNF-α. Additionally, it downregulates the expression of iNOS and COX-2 proteins, facilitating the polarization of BV-2 cells from a pro-inflammatory M1 phenotype to an anti-inflammatory M2 phenotype. Neuroprotective agent 5 also dose-dependently inhibits acetylcholinesterase (AChE) activity and the aggregation of Aβ42. This compound is useful for research into Alzheimer's disease.

Ovalitenone suppresses EMT by inhibiting the AKT/mTOR signaling pathway and shows potential in inhibiting the CSC phenotype.

TTBK1/2-IN-2 (compound 9) is a potent inhibitor of Tau tubulin kinase 1 (TTBK1) and TTBK2, with IC50 values of 384 nM and 175 nM, respectively. In human induced pluripotent stem cells (iPSC), TTBK1/2-IN-2 demonstrates a significant ciliogenesis phenotype.

HDAC6-IN-53 (Compound W28) is an inhibitor targeting histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. It reduces the idiopathic pulmonary fibrosis (IPF) phenotype by inhibiting TGF-β1-induced collagen expression and demonstrates therapeutic efficacy in a bleomycin-induced mouse model of pulmonary fibrosis. HDAC6-IN-53 is applicable for research in idiopathic pulmonary fibrosis and related pulmonary fibrotic diseases.

SIN 14 is an HO-1 activator that targets and activates HO-1 through an allosteric mechanism. Additionally, SIN 14 can induce the polarization of macrophages from the M1 phenotype to the M2 phenotype.

PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor with an IC50 of 0.79±0.09 μM. It reshapes the neutrophil phenotype, increases the proportion of dendritic cells and M1 macrophages, reduces the number of myeloid-derived suppressor cells, and enhances the tumor immune microenvironment. PAD4-IN-4 is applicable for research in triple-negative breast cancer.

JNK-IN-24 is a JNK inhibitor and an anti-metastatic cancer agent. It reduces the expression of JNK and MMP1 in cancer tissues induced by Scrib knockdown. JNK-IN-24 aids in the recovery of the ScribRNAi tumor disc phenotype and is applicable for studying various epithelial-derived cancers.

TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (with a lowest effective concentration (LEC) [hTLR7] of 1.6 μM) and TLR8 (LEC [hTLR8] of 1.6 μM). It acts on human peripheral blood mononuclear cells (hPBMC) with agonistic activity (LEC [hPBMC] = 0.5 μM). In mice and cynomolgus monkeys, TLR7/8 agonist 13 induces endogenous IFNα, activates myeloid dendritic cells and monocytes, promoting their differentiation towards a TH1 phenotype. In chronic AAV-HBV mouse models, it reduces viral load and HBV surface antigen levels. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, facilitating the response of HBV antigen-specific CD8 T cells. This compound is useful for hepatitis B virus research.

Avanbulin is a potent inhibitor of tubulin polymerization with antitumor activity. It elicits a unique microtubule (MT) phenotype, distinct from colchicine, paclitaxel, and vinblastine has broad in vitro anti-proliferative activity against a diverse range

Microtubule destabilizing agent-3 is an analogue of B32B3 and functions as a microtubule destabilizer. By destabilizing microtubules and promoting mitotic arrest, it exerts its anti-myeloma phenotype, ultimately leading to cell death. Microtubule destabilizing agent-3 induces G2/M phase arrest and caspase-dependent apoptosis (apoptosis) and can be utilized in research on multiple myeloma.