suppressive

Trilostane (Win 24540) is a synthetic androstane derivative with adrenocortical suppressive properties, reversibly inhibiting 3 beta-hydroxysteroid dehydrogenase delta [5-4] isomerase in the adrenal cortex.

OTS514 (OTS514 Hydrochloride) is a potent TOPK inhibitor. OTS514 exhibits a growth-suppressive effect on small cell lung cancer. OTS514 effectively suppressed the growth of SCLC cell lines (IC50: 0.4 ~ 42.6 nM). Treatment with OTS514 suppressed forkhead box protein M1 (FOXM1) activity. OTS514 treatment reduced CD90-positive SCLC cells and showed a higher cytotoxic effect against lung sphere-derived CSC-like SCLC cells.

αVβ8-IN-1 is an inhibitor of the αVβ8 integrin. It exhibits growth-suppressive activity against tumors such as EMT6, CT26, KPC, and TKCC-10. αVβ8-IN-1 is suitable for research related to idiopathic pulmonary fibrosis (IPF), nonspecific interstitial pneumonia (NSIP), and various cancers.

Betamethasone 17-Propionate is a compound used in the study of its effects on endotoxin-induced uveitis in rats, capable of inhibiting cellular infiltration into the aqueous humor when administered topically or systemically at certain doses. However, compared to some other compounds, its inhibitory effects are relatively weaker. When administered systemically, the dosage is 1mg kg. Additionally, in in vitro interleukin-8 (IL-8) release assays, Betamethasone 17-Propionate's suppression of IL-8 release from rat peritoneal exudate cells is less effective than that of betamethasone. Moreover, the concurrent addition of betamethasone dipropionate with Betamethasone 17-Propionate reduces the suppressive effects of betamethasone on cell infiltration and IL-1β gene expression.

CP-31398 stabilizes the active conformation of p53 in cancer cells with either mutated or wild-type p53, enhancing its activity. Additionally, CP-31398 upregulates target genes of p53 such as p21WAF1 Cip1 and KILLER DR5. This compound possesses tumor-suppressive properties.

Cofpropamine, a caffeine derivative that inhibits polyadenylation, enhances the suppressive effects of Cyclophosphamide in animal models of rat adjuvant arthritis and mouse collagen-induced arthritis.

CG500354 plays a tumor suppressive role through the cAMP/CREB signaling pathway and is a novel inducer of neural differentiation and growth arrest in primary HUMAN GBM derived cells.

Wilforlide A (3-Epiabruslactone A) is a natural product, separated from the ethanolic extract of tripterygium wilfordii. High-dose wilforlide A has obvious anti-inflammatory effect, but has no significant immune suppressive activity.

β-Endorphin (β-EP) is an endogenous opioid neuropeptide with diverse biological activities. It is produced via piomelanocortin cleavage in the pituitary gland, hypothalamus, and in lymphocytes, then migrates to its sites of action which include plasma, gut, skin, placenta, cerebrospinal fluid, and cardiac tissues. β-EP induces concentration-dependent decreases in electrically stimulated contraction of the mouse vas deferens that can be reversed by the μ-opioid antagonist CTP and δ-opioid antagonist ICI 174,864. In vivo, β-EP (5 μg, i.c.v.) slows gastrointestinal transit in mice. β-EP (0.5 or 5 μg, i.c.v.) stimulates food intake in rats for 4 to 6 hours, however, this effect is not prolonged with continuous infusion. It antagonizes the appetite-suppressive effects of α-melanocyte-stimulating hormone (α-MSH) for the first three days post administration. β-EP also reduces paralytic demyelination induced by the murine coronavirus MHV-JHM in immunocompetent, but not irradiated or immune-incompetent, mice and rats.

Destruxin B2 is a cyclic hexadepsipeptide mycotoxin that has been found in M. anisopliae and has antiviral, insecticidal, and phytotoxic activities.1,2,3 It inhibits secretion of hepatitis B virus surface antigen (HBsAg) by Hep3B cells expressing hepatitis B virus (HBV) DNA (IC50 = 1.3 μM).1 Destruxin B2 is toxic to Sf9 insect cells in an electric cell-substrate impedance sensing (ECIS) test with a 50% inhibitory concentration (ECIS50) value of 92 μM.4 It is also phytotoxic to B. napus leaves.3 |1. Yeh, S.F., Pan, W., Ong, G.-T., et al. Study of structure-activity correlation in destruxins, a class of cyclodepsipeptides possessing suppressive effect on the generation of hepatitis B virus surface antigen in human hepatoma cells. Biochem. Biophys. Res. Commun. 229(1), 65-72 (1996).|2. Male, K.B., Tzeng, Y.-M., Montes, J., et al. Probing inhibitory effects of destruxins from Metarhizium anisopliae using insect cell based impedance spectroscopy: Inhibition vs chemical structure. Analyst 134(7), 1447-1452 (2009).|3. Buchwaldt, L., and Green, H. Phytotoxicity of destruxin B and its possible role in the pathogenesis of Alternaria brassicae. Plant Pathol. 41(1), 55-63 (1992).

TEI-9648, an analogue of Vitamin D3 Lactone, acts as a potent and specific antagonist to the vitamin D receptor (VDR). This compound effectively blocks the genomic actions mediated by VDR and the Vitamin D responsive element (VDRE) of 1α,25(OH)2D3. Furthermore, TEI-9648 prevents the differentiation of HL-60 cells induced by 1α,25(OH)2D3, indicating its utility in bone metabolism studies[1][2].

4-Maleimidosalicylic acid, a polar maleimide compound, does not suppress IL-2 production in JURKAT T cells.

D-(+)-Sorbose, the active enantiomer of D-Sorbose, inhibits disaccharidase activity and demonstrates suppressive effects on postprandial blood glucose and insulin levels in rats. Its role as a sweetener may aid in preventing lifestyle-related diseases, such as type 2 diabetes mellitus.

FLDP-5, a blood-brain barrier (BBB) penetrant curcuminoid analogue, induces the production of Reactive Oxygen Species (ROS), DNA damage, and cell cycle S phase arrest. It demonstrates significant tumor-suppressive effects, exhibiting potent anti-proliferative and anti-migratory activities on LN-18 cells.

(Rac)-Mono(3,5,5-trimethylhexyl) phthalate, a notable metabolite of commonly used phthalate plasticizers, displays immuno-suppressive effects [1].

Tregalizumab, a humanized IgG1-type monoclonal antibody targeting CD4, selectively activates regulatory T cells (Tregs) with suppressive functions in vitro and has potential applications in researching autoimmune diseases (due to inadequate Treg activity) and allergies [1] [2] [3].

Topsalysin, a prostate-specific antigen (PSA)-activated protoxin, comprises a synthetic proaerolysin fusion protein targeting human prostate-specific antigen. This compound has demonstrated tumor-suppressive effects in a mouse model [1].

Pancreastatin (33-49), porcine, a peptide fragment derived from the porcine pancreas, exerts insulin-suppressive effects in vitro and augments the glucose priming effect [1] [2].

Laxiflorin B-4, a derivative of Laxiflorin B, demonstrates increased affinity for ERK1 2 and enhanced tumor-suppressive effects [1].

CKS-17, a synthetic retroviral envelope peptide, embodies conserved amino acid sequences found in the transmembrane envelope proteins of various animal and human retroviruses. This immunomodulatory epitope exerts suppressive effects on a range of immune functions [1] [2] [3].

M1069 (free base) is an orally active and selective dual antagonist for the A2A and A2B adenosine receptors, demonstrating over 100-fold selectivity compared to A1 and A3 receptors. It mitigates the immune-suppressive effects of adenosine and shows anti-tumor properties [1] [2] [3].

STAT3-IN-32 (compound 4c) is an orally active, potent dual phosphorylation inhibitor of STAT3. It demonstrates significant inhibition of STAT3 luciferase activity in HEK293T cells, with an IC50 of 5.3 nM, and inhibits ATP production in BxPC-3 cells with an IC50 of 4.2 nM. By targeting the STAT3 SH2 domain (KD=21.3 nM), STAT3-IN-32 effectively blocks p-Tyr705 and p-Ser727, leading to the attenuation of STAT3 nuclear transcription and mitochondrial oxidative phosphorylation. Furthermore, this compound displays notable suppressive effects in a pancreatic cancer xenograft model.

eEF2K degrader-1 is a degrader of eEF2K, known to inhibit the viability, proliferation, and migration of MDA-MB-231 and HCC1806 cell lines, with an IC50 value of 43.71 nM in MDA-MB-231 cells. Furthermore, eEF2K degrader-1 demonstrates tumor-suppressive effects in a xenograft mouse model using MDA-MB-231 cells.

WQQ-345, a BCAT1 inhibitor, exhibits an IC50 of 10.8 mM. In 67R cells, it reduces α-KG levels and upregulates H3K27me3 expression while downregulating the expression of glycolytic enzymes (PFKP and LDHA), leading to impaired glycolytic activity. Additionally, WQQ-345 demonstrates tumor-suppressive activity in a 67R subcutaneous xenograft model.