phenotype

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.

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

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

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 sensitize. BMOV is 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, respectivelyr[1][2].

IGF-1R inhibitor-2 (example 121) is a compound that inhibits the insulin-like growth factor-1 receptor (IGF-1R). By downregulating the IGF-1R, it has the potential to reverse the transformed phenotype of tumor cells and make them more susceptible to apoptosis.

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

Highly selective orally active peroxisome proliferator-activated receptor (PPAR)γ agonist (pEC50 values are 8.05, < 4 and < 4 for human PPARγ, PPARα and PPARδ receptors respectively). Decreases glucose, fatty acid and triglyceride levels following oral administration in vivo. Brown et al (1999) A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-γ reverses the diabetic phenotype of the Zucker diabetic fatty rat. Diabetes 48 1415 PMID:10389847 |Nugent et al (2001) Potentiation of glucose uptake in 3T3-L1 adipocytes by PPARγ agonists is maintained in cells expressing a PPARγ dominant-negative mutant: evidence for selectivity in the downstream responses to PPARγ activation. Mol.Endocrinol. 15 1729 PMID:11579205 |Way et al (2001) Adipose tissue resistin expression is severely suppressed in obesity and stimulated by peroxisome proliferator-activated receptor γ agonists. J.Biol.Chem. 276 25651 PMID:11373275

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

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.

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.

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.

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.

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

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.

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.

ERD03, with a dissociation constant (Kd) of 17±7 μM, effectively disrupts the EXOSC3-RNA interaction. It has been shown to induce a PCH1B-like phenotype in zebrafish embryos, making it a valuable tool for research into neurological disorders [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.

DC-BPi-03 is a novel BPTF-BRD inhibitor (IC50 of 698.3 nM) with a potential anticancer phenotype for leukemia research.

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

Tonantzitlolone is a natural agonist of tprc1/4/5 channels, also acting as a dual pkcα and pkcθ activator, inducing an insulin resistant phenotype by inhibiting irs1 and the pi3k/akt pathway, activating the heat shock factor 1 (hsf1) transcription factor driving glucose dependency

FKBP51F67V-selective antagonist Ligand2 (example 3-3), a potent ligand, selectively binds to the FKBP51 F67V variant, with no affinity for wild-type FKBP51 or FKBP52 [1]. It effectively reverses the anxiogenic phenotype resulting from FKBP51 F67V overexpression in the amygdala.

P-gp inhibitor 5 is a potent inhibitor of P-glycoprotein (P-gp), inhibiting P-gp by a factor of 2.5 and 3.0 at 1.25 μM and 2.5 μM, respectively. p-gp inhibitor 5 exhibits anti-proliferative effects on some cancer cells. P-gp inhibitor 5 was able to restore cellular sensitivity to Vincristine and Paclitaxel, thereby reversing the multidrug resistant (MDR) phenotype of ABCB1/Flp-InTM-293 and KBvin.

GS-9822 is a novel LEDGIN, an inhibitor that targets the binding pocket of LEDGF/p75 which is a cellular cofactor that substantially contributes to HIV integration site selection, displaying a block-and-lock phenotype in cell culture.

2,4,5-Trimethoxybenzoic acid is a compound identified in purple perilla extracts that inhibits M1 macrophage phenotype-mediated inflammation in diabetes [1].

ALV2 is a potent and selective Helios degrader compound that binds to the CRBN protein, exhibiting an IC50 value of 0.57 μM. Helios, a zinc-finger transcription factor, plays a crucial role in preserving a stable T reg cell phenotype within the inflammatory tumor microenvironment.

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).

BMS-186511 is a Farnesyltransferase (FT) inhibitor with potential anticancer activity. BMS-186511 is a bisubstrate analogue inhibitor of FT, would inhibit the malignant growth properties of a cell line established from malignant schwannoma of an NF1 patient. Following treatment with BMS-186511 , ST88-14 cells became flat, nonrefractile, were contact-inhibited, and lost their ability to grow in soft agar. BMS-186511 was found to specifically inhibit FT, but not geranylgeranyltransferase I, a closely related enzyme. Thus, it is conceivable that FT inhibitors may ultimately become the first generation of drugs against the malignant phenotype in NF1 based on rational insights into the mechanism of action of neurofibromin.

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

Anti-neuroinflammation Agent 1 effectively modulates BV2 microglia cell polarization, shifting from an M1 to an M2 phenotype [1].

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

Osteocalcin (1-49) is a non-collagenous peptide that is secreted by osteoblasts and odontoblasts and comprises 1-2% of the total protein in bone. Secretion of osteocalcin (1-49) is stimulated by 1,25-dihydroxy vitamin D and plasma levels increase in diseases that induce dysregulated bone turnover such as osteoporosis, Paget's disease, and primary hyperparathyroidism. Osteocalcin (1-49) is positively correlated with insulin sensitivity and negatively correlated with high blood glucose levels in women. In vitro, osteocalcin induces chemotaxis of MDA-MB-231 breast cancer cells, human peripheral blood monocytes, and rat osteosarcoma cells with osteoblast-like characteristics. It is also expressed by vascular smooth muscle cells (VSMCs) displaying an osteoblast-like phenotype and has been positively associated with calcification of aortic tissue and heart valves in humans.

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