si-2

SI-2 is an inhibitor (SMI) of steroid receptor coactivator-3 (SRC-3 or AIB1). SI-2 can selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells, and selectively induce breast cancer cell death with IC50 values in the low nanomolar range (3-20 nM), but not affect normal cell viability.

(E)-SI-2 is a potent small-molecule inhibitor of steroid receptor coactivator-3 (SRC-3 or AIB1) that can selectively inhibit the intrinsic transcriptional activities of SRC-3, also inhibits SRC-1 and SRC-2. It selectively reduces cellular protein levels of SRC-3, but not that of CARM-1, blocks MDA-MB-468 cell growth with an IC50 value of 3.4 nM, but spares normal cells.

SI-2 hydrochloride (EPH 116 hydrochloride) is a highly promising inhibitor of SRC-3 SMI: SRC-3 (PPI)(IC50 values of 3-20 nM for breast cancer cell death), with acceptable oral availability.

OSI-296 is a potent and dual inhibitor of cMET and RON kinases (IC50 value are 42 nM and 200 nM for cMet and sfRon respectively) . OSI-206 shows in vivo efficacy and is well tolerated in tumor xenografts models upon oral dosing. OSI-296 also reduces tumou

OXSI-2 (Syk Inhibitor) is an inhibitor of Syk with an EC50 of 313 nM and an IC50 of 14 nM. OXSI-2 completely inhibits Adaptor protein LAT Y191 phosphorylation and Syk mediated events in platelets.

MEISi-2 Dihydrochloride is a useful organic compound for research related to life sciences and the catalog number is T35370.

ASI-254 is an aminosugar cardiac glycoside and an inhibitor of Na+,K+ -ATPase.

G12Si-2, an analog of G12Si-1 , is a negative control tool. G12Si-2 is not a covalent inhibitor of the G12S mutant of K-Ras [1] .

MEISi-2 is a specific MEISi inhibitor that inhibits the meis luciferase reporter gene in vitro and induces MEIS-dependent hematopoietic stem cell maintenance and self-renewal, which can be used in research areas such as cardiac injury, hematopoietic problems, bone marrow transplantation and cancer.

Apicidin (OSI 2040) is a histone deacetylase (HDAC) inhibitor with antiparasitic and antiproliferative activity. It attenuates memory deficits, inhibits cell growth and proliferation, and induces apoptosis and autophagy by decreasing Abeta load in APP/PS1 mice, making it a valuable tool for leukemia research.

HMS-I2 is a chemical probe used to form heterochromatin. It works by disrupting heterochromatin mediated transcriptional gene silencing.

Semapimod tetrahydrochloride (CPSI-2364 tetrahydrochloride) is a synthetic ornithine mitogen-activated protein kinase blocker and pro-inflammatory cytokine production inhibitor that interferes with macrophage and microglia function. Sematimod tetrahydrochloride inhibits TLR4 signaling, TNF-α, IL-1β, and IL-6, and is used in the study of Crohn's disease and other inflammatory conditions.

Lurtotecan (GI147211) is a semisynthetic Camptothecin analog. Lurtotecan is a topoisomerase I inhibitor with anticancer effects.

Iniparib (BSI-201) (BSI-201) , a PARP1 inhibitor, exhibits potency in triple-negative breast Y (TNBC).

Semapimod is an inhibitor of proinflammatory cytokine production, capable of suppressing TNF-α, IL-1β, and IL-6. It hinders TLR4 signaling with an IC50 of approximately 0.3 μM, impedes p38 MAPK, and reduces nitric oxide production in macrophages. This compound shows promise for treating various inflammatory and autoimmune disorders [1] [2] [3].

Beauveriolide III, a cyclodepsipeptide found in Beauveria fungi, inhibits lipid droplet formation (at 3-10 μM) and cholesterol synthesis (IC50=0.41 μM). This compound also suppresses acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity (IC50=5.5 μM) and reduces atherosclerotic lesion size in Ldlr-/- and ApoE-/- mouse models (25-50 mg/kg).

HIV-1inhibitor-79 (Compound 3k) is an HIV inhibitor that demonstrates significant inhibitory activity against HIV-1 and its common mutants, with IC50 values of 1.9 nM for HIV-1, K103, 8.7 nM for L100I, and 11 nM for E138K. It exhibits low cytotoxicity and a high selectivity index (CC50 = 21.95 μM, SI = 11478). Additionally, HIV-1inhibitor-79 shows antiviral activity against HIV-2, with an EC50 value of 6.14 μM, and effectively inhibits HIV-1 reverse transcriptase with an IC50 of 25 nM.

SARS-CoV-2-IN-110 (compound Bb1) is an inhibitor of SARS-CoV-2, demonstrating antiviral efficacy with an EC50 of 1.10 μM, and significantly reduced toxicity compared to Lapatinib. The compound exhibits a CC50 of greater than 100 μM against SARS-CoV-2, with a selectivity index (SI) exceeding 91.

Scr-IN-1 (Compound 4e) is a tyrosine kinase inhibitor demonstrating inhibitory activity against HCT-116 and MIA-PaCa-2 cells, with IC50 values of 0.16 μM and 1.16 μM, respectively. It shows selectivity towards HCT-116 cells and MIA-PaCa-2 cells, with a selectivity index (SI) greater than 625 and 86. Scr-IN-1 induces apoptosis in HCT-116 colon cancer cells without altering the proportion of necrotic cells and is a potential novel SRC kinase inhibitor for HCT-116 cells. This compound is suitable for cancer research.

SRC-3-IN-2 (SI-12 6c) is an orally active inhibitor of steroid receptor coactivator 3 (SRC-3) with antitumor properties.

STINGDegrader-2 (Compound SI-43) is an inhibitor and mutant-specific degrader of STING. It effectively suppresses cGAMP-induced STING activation and significantly reduces the release of IFN-β and CXCL-10. By binding to two pockets of the STING dimer, it inhibits activity and induces proteasome-independent degradation of the mutant STINGS154 and STINGM155 (DC50 values of 0.31 and 0.76 μM, respectively). STINGDegrader-2 is applicable in the study of STING-related autoimmune diseases.

Beauveriolide I is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.78 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide I also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 6 μM).2 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

VV116 is a selective and orally active nucleoside antiviral agent against respiratory syncytial virus and SARS-CoV-2 infection.[1]

Caffeoylcalleryanin demonstrated potent inhibitory activity against 15-lipoxygenase (15-LOX), with an IC50 value of 1.59 μM. Furthermore, ethanol extract from A. pulchra leaves (EEAPL) was found to contain compounds exhibiting antiviral properties, particularly effective against Dengue virus type 2 (DENV-2). Among these compounds, Caffeoylcalleryanin emerged as the most potent anti-DENV-2 agent, achieving a selectivity index (SI) of 20.0.