selective

MPI_5a is an effective and selective inhibitor of HDAC6 (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms and it also inhibits acyl-tubulin accumulation in cells (IC50: 210 nM).

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.

Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.

DFP00173 is a potent and selective aquaporin 3 (AQP3) inhibitor, with an IC50 of approximately 0.1-0.4 μM for both mouse and human AQP3. It demonstrates selectivity for AQP3 compared to homologous AQP subtypes AQP7 and AQP9.

SB 258719 is a selective antagonist of 5-HT7 receptor(pKi of 7.5).

TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1)(IC50 of 14 nM).

NHWD-870 is an effective and selective inhibitor of BET family bromodomain only binding to BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. NHWD-870 exhibits potent anti-tumor efficacies and suppresses cancer cell-macrophage interaction through the increase of tumor apoptosis and inhibition of tumor proliferation.

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.

Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.

Spironolactone (SC9420) is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.

Fenclonine (CP-10188) is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine(CP-10188) acts pharmacologically to deplete endogenous levels of serotonin.

Bazedoxifene acetate (WAY-TES 424) is a novel selective estrogen receptor modulator (SERM).

Vardenafil hydrochloride trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

Vardenafil hydrochloride is a New Phosphodiesterase Type 5(PDE5) Inhibitor, in the Treatment of Erectile Dysfunction in Men With Diabetes

JNJ-39758979 is a selective and high-affinity histamine H4 receptor antagonist (Kis: 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively). JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2

4F 4PP oxalate is a 5-HT2A antagonist.

Slingshot inhibitor D3 (JHN76359) is a potent inhibitor of the Protein Phosphatase Slingshot.

(Rac)-SAR131675 is an effective and specific VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity (IC50: 20 nmol/L) and VEGFR-3 autophosphorylation (IC50: 45 nmol/L) in HEK cells, respectively. SAR131675 is highly specific for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is a highly specific VEGFR-3-TK inhibitor with significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.

GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).

TCN 213 is an antagonist of NMDA receptor that has a selective for NR1/NR2A over NR1/NR2B

BMS-986242 is an orally active, potent, and selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor, suitable for cancer research.

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor that inhibits BRD4 with an IC50 of 5193nM.

BAY-1797 is an orally active and selective P2X4 antagonist (IC50: 211 nM against human P2X4) with anti-nociceptive and anti-inflammatory effects. BAY-1797 displays no or very weak activity on the other P2X ion channels.