BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.

DC-05 is a selective, non-nucleoside DNA methyltransferase DNMT1 inhibitor with IC50 of 10.3 uM, displays 3.6-fold selectivity over PRMT1 and >15-fold over DNMT3A, DNMT3B, G9a, SUV39H1, MLL1, SET7/9..

C16, also known as GW-506033X or PKR Inhibitor. C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM. GW-506033X protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress. PKR inhibitor C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component. PKR inhibitor C16 binds efficiently with human microtubule affinity-regulating kinase 4.

Triazavirin is a guanine nucleotide analog antiviral originally developed in Russia that has shown efficacy against influenza A and B, including the H5N1 strain. It appears that Triazavirin has shown promise in reducing influenza disease severity and associated complications.5 Given the similarities between SARS-CoV-2 and H5N1, health officials are investigating Triazavirin as an option to combat SARS-CoV-2, the coronavirus responsible for COVID-19.

An E3 ligase ligand-linker conjugate for PROTAC..

SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist.

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.