si 2

(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.

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.

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] .

(1R,2R)-ML-SI3 ((-)-trans-ML-SI3) is a selective TRPML1, TRPML2, and TRPML3 inhibitor for the study of neurodegenerative and cardiovascular diseases.

(1S,2S)-ML-SI3, the trans-isomer of ML-SI3, acts as a TRPML inhibitor. This (-)-isomer effectively inhibits TRPML1 and TRPML2 with IC 50 values of 1.6 μM and 2.3 μM, respectively, and exhibits weaker inhibition of TRPML3 with an IC 50 of 12.5 μM. In contrast, the (+)-enantiomer inhibits TRPML1 (IC 50 = 5.9 μM) and serves as an activator for TRPML2 and TRPML3 with EC 50 values of 2.7 μM and 10.8 μM respectively [1].'

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

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.

ASI-222 is an aminoglycoside cardiotonic compound. It functions by inhibiting sodium-potassium ATPase (Na+/K+ ATPase) and exhibits positive inotropic effects. ASI-222 can be utilized in cardiovascular disease research.

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.

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

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

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).

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

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].

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.

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

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.