i1

6α-Prostaglandin I1 (6α-PGI1) is a stable Prostaglandin I2 (PGI2) analog resistant to hydrolysis in aqueous solutions. It promotes cyclic AMP accumulation in human thyroid slices and cells in a concentration-dependent manner but is about 10-fold less potent than the β-isomer and 100-fold less potent than PGI2 in eliciting this response. 6α-PGI1 exhibits an IC50 of 350 ng/ml for inhibition of ADP-induced platelet aggregation, nearly 900-fold higher than that of PGI2 (0.4 ng/ml).

PCNA-I1 is an inhibitor targeting PCNA chromatin association in prostate cancer.

Rilmenidine hemifumarate (S-3341 hemifumarate) is a novel, orally active and selective I1 imidazoline receptor and α2-adrenoceptor agonist that induces autophagy, regulates the proliferation of leukaemia cells, stimulates the pro-apoptotic protein Bax, and induces autophagy in human leukaemia K5 cells. induces disruption of the mitochondrial pathway and apoptosis in human leukaemia K562 cells.

Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist, used to treat hypertension.

6β-PGI1 is a stable PGI2 analog resistant to hydrolysis in aqueous solutions. 6β-PGI1 has a much longer half-life than PGI2, but a greatly reduced molar potency for receptor mediated function. 6β-PGI1 has a Kact for adenylate cyclase in NCB-20 cells of 4.2 μM compared with 18 nM for PGI2. The potency for vasodilation and inhibition of platelet aggregation is about 1% of PGI2.

Harmane (Loturine) is a bio-active β-Carboline and monoamine oxidase inhibitor found in coffee and tobacco smoke.

JI130 is able to impair the ability of Hes1 to repress transcription. JI130 treatment significantly reduced tumor volume in a murine pancreatic tumor xenograft model.

HPi1 is a selective and orally active antimicrobial against Helicobacter pylori (IC50: 0.24 μM and a MIC of 0.08-0.16 μg/mL). HPi1 is inactive against other Xaliproden, including the gut commensals, Lactobacillus reuteri, Lactobacillus casei, and Bifidoba

NSI189 (NSI-189) is a nootropic and neurogenic research chemical derived from nicotinamide and pyrazine.

O4I1 is an effective Oct3/4 inducer.

CPI1189 (REN-1189) is a TNF-a release inhibitor potentially for the treatment of sciatica and postherpetic neuralgia.

Phox-I1 is a NOX2 inhibitor targeting the interactive site of p67phox with Rac GTPase.

HMS-I1 Hydrobromide is a probe that works by destroying heterochromatin mediated transcriptional gene silencing and is used for studies of heterochromatin formation and function.

(+)-CBI-CDPI1, an enhanced functional analog of CC-1065, is a DNA alkylating agent and an antibody-drug conjugate (ADCs) toxin.

NCI172112 is is used to develop antitumor agents effective against CNS tumors.

NMDI14 is an inhibitor of nonsense mediated RNA decay (NMD).

NIK SMI1 is an effective and selective NF-κB inducing kinase (NIK) inhibitor. It also inhibits NIK-catalyzed hydrolysis of ATP to ADP (IC50: 0.23±0.17 nM).

ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4, also degrades the polybromo-associated BAF (PBAF) complex member PBRM1, with DC50s of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 can induce anti-proliferative effects and apoptosis.

ESI1 is a small molecule inhibitor of epigenetic silencing. This compound induces the formation of nuclear aggregates of the key lipid metabolism regulator SREBP1/2, thereby concentrating transcription co-activators to drive lipid/cholesterol biosynthesis. Additionally, ESI1 promotes myelin regeneration in demyelination animal models and facilitates de novo myelination on regenerating CNS axons, reversing age-related cognitive decline.

BI1543673 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4). It can diminish inflammatory responses in human lung tissue stimulated by TLR4 and TLR7/8. Additionally, BI1543673 reduces inflammatory signaling in a mouse lung inflammation model induced by LPS.

CBI1 formic is a covalent inhibitor of BAX, selectively derivatizing BAX at C126 and inhibiting its activation by triggering with a ligand or point mutation. This compound effectively blocks the t-2-hex lipidation and oligomerization of BAX. Additionally, CBI1 formic inhibits BAX activation induced by BH3 ligands, F116A mutations, or t-2-hex.

I194496 is an effective inhibitor of cystathionine γ-lyase (CSE) with an IC50 value of 0.79 mM. It inhibits the growth of human TNBC cells by dual targeting the PI3K/Akt and Ras/Raf/ERK pathways. Additionally, I194496 suppresses the metastasis of human TNBC cells by downregulating the Anxa2/STAT3 and VEGF/FAK/Paxillin signaling pathways.

RKI1313 (RKI-1313) was a selective inhibitor for ROCK-dependent signaling, cytoskeletal changes, anchorage-independent colony formation, migration, and invasion.

BI1701963 is an orally effective inhibitor that targets the SOS1 and KRAS interaction, specifically inhibiting the activation of KRAS by blocking its GTP loading. This compound is utilized in cancer research to explore potential therapeutic effects against KRAS-driven malignancies.