phenotype

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

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

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.

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].

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

IGF-1R inhibitor-2 (example 121) is a compound that inhibits the insulin-like growth factor-1 receptor (IGF-1R), potentially reversing the transformed phenotype of tumor cells and increasing their susceptibility to apoptosis.

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

KHS101 is a TACC3 inhibitor and can selectively induce a neuronal differentiation phenotype.

SNU-BP is an agonist of PPAR-gamma, inhibiting lipopolysaccharide (LPS)-induced NO production and pro-inflammatory cytokines. SNU-BP potentiates interleukin-4-induced arginase-1 expression, and promotes microglial polarization toward an M2 anti-inflammatory phenotype.

CHD1Li 6.11 is a potent inhibitor of oncogenic CHD1L, acting on the cat-CHD1L recombinant protein (IC50: 3.3 μM). CHD1Li 6.11 is an orally active antitumour agent that significantly reduces the tumour volume of CRC xenografts generated from isolated quasi-mesenchymal cells (M phenotype) with enhanced tumourigenic properties. These cells have enhanced tumourigenic properties.

MK2-IN-6 (Compound 11) is an effective and selective irreversible inhibitor of MK2 with an IC50 value of 2.3 nM. It suppresses the kinase activity of MK2, leading to sustained inhibition of MK2 signaling and reduction of pathological inflammatory factors in macrophages. MK2-IN-6 is capable of inhibiting the M2-like protein phenotype in macrophages both in vitro and in vivo, showing potential for use in colorectal cancer research.

2-Fluoropalmitic acid (2-Fluorohexadecanoic acid), a fatty acid containing fluorine atoms, serves as a potential therapeutic agent for glioblastoma (GBM) by inhibiting the viability, proliferation, and stem-like phenotype of glioma stem cells (GSCs), suppressing the expression of phosphorylated erk, CD133, and SOX-2, and leading to decreased MMP-2 activity and increased methylation of the MGMT promoter.

L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist, activates AHR-driven polarization of naive T cells towards the anti-inflammatory [Treg] phenotype.

BMS-214662 is a Farnesyltransferase inhibitor , is also a nonsedating benzodiazepine derivative with potential antineoplastic activity. BMS-214662 inhibits the enzyme farnesyltransferase and the post-translational farnesylation of number of proteins involved in signal transduction, which may result in the inhibition of Ras function and apoptosis in susceptible tumor cells. This agent may reverse the malignant phenotype of H-Ras-transformed cells and has been shown to be active against tumor cells with and without Ras mutations.

XR3054 is a novel inhibitor of farnesyl protein transferase (FPTase). XR3054 inhibited the proliferation of the prostatic cancer cell lines LnCAP and PC3 and the colon carcinoma SW480 and HT1080 (IC50 values of 12.4, 12.2, 21.4 and 8.8 microM, respectively) but was relatively inactive when tested against a panel of breast carcinoma cell lines. The activity did not relate to the presence of mutant or wild-type ras in the cell lines tested. In conclusion XR3054 inhibits ras farnesylation, MAP kinase activation and anchorage-independent growth in NIH 3T3 transformed with v12 H-ras. Since the antiproliferative effect of the compound is not related to the ras phenotype, XR3054 may also have effects on other cell signaling mechanisms.

XR9051 is as a potent modulator of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) following a synthetic chemistry programme based on a natural product lead compound. XR9051 was shown to be a potent inhibitor of the binding of the cytotoxic to P-glycoprotein (EC50 = 1.4 + - 0.5 nM). XR9051 reverses the MDR phenotype through direct interaction with P-glycoprotein.

Bexmarilimab (FP-1305) is a highly potent, humanized anti-CLEVER-1 IgG4 antibody with an IC50 value of 4.51 nM, promoting immune conversion of tumor-associated macrophage phenotype M2 to M1, and can be used to study cancer.

Sakura 6, a synthetic serotonin transporter (SERT)-binding peptide, enhances the interaction between SERT and neuronal nitric oxide synthase. This interaction decreases SERT activity and its presence on the cell surface, augments auto-inhibition, lowers synaptic 5-HT release, and diminishes activity in the dorsal raphe nucleus, ultimately inducing an acute depressive phenotype in a mouse depression model.

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.

CSF1R-IN-22 (Compound C19), a potent orally administered CSF-1R selective inhibitor (IC50 <6 nM), significantly enhances CXCL9 secretion from M2 macrophages and promotes CD8+ T cell infiltration. Moreover, it amplifies the anti-tumor immune responses in conjunction with anti-PD-1 and triggers apoptosis in tumor cells. Additionally, CSF1R-IN-22 effectively reprograms M2-like TAMs (tumor-associated macrophages) to an M1 phenotype, modulates the tumor microenvironment (TME) by fostering the recruitment of CD8+ T cells, and diminishes the presence of immunosuppressive Tregs and MDSCs [1].

Hexafluoro is an inhibitor of DRP1 phosphorylation. Honokiol DCA stimulates a phenotype suggestive of respiration through mitochondrial normalization and demonstrates activity in Vemurafenib-resistant melanoma in vivo.