HLY78 is an activator of the Wnt/β-catenin signaling pathway, which targets the DIX domain of Axin and potentiates the Axin-LRP6 association to promote Wnt signaling transduction[1].

FB23 is a potent and selective FTO demethylase inhibitor with an IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N6-methyladenosine (m6A) demethylase activity.

WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2.1,2 It is a much weaker inhibitor of phosphatidylinositol 3-kinase α (IC50 = 1026 nM) and other kinases.3 WYE-354 i

N-desmethyl Enzalutamide(N-desmethyl MDV3100) is a major metabolite of Enzalutamide, Enzalutamide(MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.

NIK SMI1 is a potent, selective small molecule inhibitor of NF-κB inducing kinase (NIK) with Ki of 230±170 pM; only inhibits 3 out of 222 off-target kinases (KHS1, LRRK2, and PKD1) with >75% inhibition at 1 uM; potently inhibits anti-LTβR-induced nuclear p52 levels in anti-LTβR-stimulated HeLa cells, with no effect on canonical signaling; inhibits BAFF and CD40 signaling, suppresses immune responses in vivo; suppresses disease biomarkers and improves survival and renal function in NZB/W F1 mice.

CYM50308 is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.

Unique F-box/LRR-repeat protein 2 (FBXL2) activator

BMS 191011 is an activator of large-conductance calcium-activated potassium (BKCa) channels that increases maximum potassium current to 126% of control in X. laevis oocytes expressing human BKCa channels when used at a concentration of 1 μM.

PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

LY-487379 is a potent, selective positive allosteric modulator of mGluR2 (EC50=0.27 uM) without activity at mGluR3; shows no intrinsic agonist or antagonist activity at hmGluR2, markedly potentiates glutamate-stimulated [35S]GTPgammaS binding at hmGluR2; potentiates synaptically evoked mGluR2 responses in rat hippocampal slices, modulates excitatory synaptic transmission in the rat globus pallidus.

Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.

CRT5 is a pyrazine benzamide that prevents activation of all three isoforms of PKD in endothelial cells treated with VEGF (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively).

BMS-189453 (BMS189453, BMS453) is a synthetic retinoid that acts as an agonist of RARβ and an antagonist of RARα and RARγ.

RO2959 is a novel, potent and selective CRAC current inhibitor. RO2959 completely inhibited cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction). RO2959 potently blocked TCR triggered gene expression and T cell functional pathways similar to CsA and another calcineurin inhibitor FK506.

TCPOBOP is an agonist of the constitutive androstane receptor (CAR) (EC50 = 20 nM). TCPOBOP enhances the nuclear receptor CAR transactivation of cytochrome P450 (CYP), as dose-dependent direct agonist of CAR. The most potent known member of the phenobarbital-like class of CYP-inducing agents. TCPOBOP has been used for enhancing Mcl-1-Italics promoter functions in mouse hepatoma cells. TCPOBOP has also been used to study constitutive androstane receptor(CAR)-induced gene expression in mouse hepatocytes.

A potent, selective inhibitor of human LIMK1 with IC50 of 38 nM .

PF-05150122 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5..

LGD-2226 (LGD2226) is an orally active, selective androgen receptor modulator (SARM) with binding Ki of 1 nM, >1000-fold selectivity over GR,PR, MR and ER.

Pyrrolnitrin is an antibiotic isolated from Pseudomonas pyrrocinia. Pyrrolnitrin shows a broad spectrum of antibiotic activity against fungi, yeast and gram-positive bacteria.

AX-024 is an cytokine release inhibitor which can strongly inhibit the production of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10 and IL-17A.

BIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM.

FT011 is an anti-fibrotic agent, reduces mRNA expression of collagens I and III and inhibits collagen synthesis.

A small molecule inhibitor of PSD-95/nNOS interaction with IC50 of 31 uM, without inhibiting nNOS catalytic activity.

JNJ 42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor.

A potent and selective GlyT1 inhibitor with IC50 of 15.8 nM, displays no activity for GlyT2 (IC50>30 uM).

SKF38393 HCl is a selective dopamine D1/D5 receptor agonist.

Tirapazamine is an experimental anticancer drug that is activated to a toxic radical only at very low levels of oxygen (hypoxia). Such levels are common in human solid tumors, a phenomenon known as tumor hypoxia.

TCS 401 is a potent, selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B) with Ki of 0.29 uM, weakly inhibits the protein phosphatases CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1, and LAR D1D2 with Ki of 59, 560, 1,100, >2,000, >2,000, and >2,000 u

Azeliragon 2HCl (also known as TTP488 2HCl and PF-04494700 2HCl) is a potent and orally bioactive RAGE (Receptor for Advanced Glycation End products) inhibitor that has the potential for the treatment of mild-to-moderate Alzheimer's disease and cerebral amyloid angiopathy. RAGE is a pattern recognition receptor that affects the movement of amyloid (a biomarker for Alzheimer's disease) into the brain. In preclinical studies, azeliragon decreased brain amyloid in mice and improved their performance on behavior tests. Azeliragon has been shown to be involved in adaptive immune responses. It is currently in Phase 3 clinical trial.

SAR405 is a highly potent and selective PI3K class III isoform Vps34 inhibitor with IC50 of 1.2 nM, inhibits the formation of autophagosomes in GFP-LC3 cells with IC50 of 4 nM.