Formamide (Methanamide; Formimidic acid) is a clear liquid amide derived from formic acid. It allows for the denaturation and renaturation of nucleic acids at room temperature. Formamide-induced DNA denaturation when combined with detection of denatured DNA with a monoclonal antibody (MAb) makes it possible to specifically identify the apoptotic cells.

Methoxyamine is an orally bioavailable small molecule inhibitor with potential adjuvant activity. Methoxyamine covalently binds to apurinic/apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER), which may result in an increase in DNA strand breaks and apoptosis. This agent may potentiate the anti-tumor activity of alkylating agents. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity.

A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.28 uM.

Novel inhibitor of MuRF1, attenuating skeletal muscle atrophy and dysfunction in cardiac cachexia

MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer[1][2].

ALLO-2 is a potent small molecule Smoothened (Smo) antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.

JNK-IN-7 is a relatively selective JNKs inhibitor(IC50= 1.54/1.99/0.75 for JNK1/2/3); also bound to IRAK1, PIK3C3, PIP5K3 and PIP4K2C.

Euquinine is generally used as a febrifuge, antimalarial, and tonic.

Cefotetan Sodium, also known as ICI-156834 and YM-09330, is a second-generation cephalosporin, cephamycin antibiotic that is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative bacteria. Cefotetan binds to penicillin-binding proteins and disrupts the cell wall synthesis.

JNJ-53718678 (JNJ53718678, JNJ-678) is a potent (Kd=7.4 nM), small-molecule inhibitor of the F-glycoprotein-mediated complex membrane fusion process of the RSV.

PF-06446846 (PF-6446846) is a potent, highly selective inhibitor of PCSK9 translation with IC50 of 0.3 uM for inhibition the secretion of PCSK9 by Huh7 cells.

SM-7368 inhibits TNF-alpha-induced MMP-9 upregulation in a concentration-dependent manner. SM-7368 strongly inhibits the TNF-alpha-induced invasion of HT1080 human fibrosarcoma cell line.

KCC-07 is a potent, selective and brain-penetrant inhibitor of MBD2 (methyl-CpG-binding domain protein 2) with anticancer activity. It prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling.

dBRD9 dihydrochloride is a potent and selective degrader (PROTAC) of BRD9 with IC50 of 56.6 nM in MOLM-13 cells.dBRD9 is composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide.dBRD9 does not degrade BRD4 or BRD7 at concentrations up to 5 uM.dBRD9 exhibits antiproliferative effects in human AML cell lines.

MS023 hydrochloride is a potent, selective and cell-active inhibitor of human type I protein arginine methyltransferases (PRMT), with IC50 values of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.

UZH2 is a potent and selective METTL3 inhibitor with an IC50 value of 5 nM.

A cell-permeable, small-molecule c-Abl kinase activator with pEC50 of 6.1(EC50=794 nM).

ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. ELN-441958 is highly selective for B1 over B2 receptors, and >500/ 2000-fold selective for the B1 over μ/δ-opioid receptor.IC50 value: 0.26 nM (Ki)Target: B1 Receptorin vitro: ELN-441958 is a novel small molecule bradykinin B1 receptor antagonist, based on the inhibition of agonist-induced increases in intracellular calcium in native and recombinant cells. ELN-441958 does not inhibit the activation of the human bradykinin B2 receptor at concentrations up to 10 μM, showing that it is highly selective for B1 over B2 receptors. ELN-441958 also displays good selectivity for B1 over other receptors examined in a broad screening panel. It is >500-fold and >2000-fold selective for the B1 receptor over the human μ- and δ-opioid receptor, the most potent off-target activity identified. In IMR-90 cells expressing the native human B1 receptor, ELN-441958 produced a concentration-dependent antagonism of the DAKD-induced calcium mobilization with a KB of 0.12 nM. [1]in vivo: ELN-441958 is essentially completely absorbed and produces high plasma levels after oral administration in rhesus monkeys.ELN-441958 has a moderate clearance and volume of distribution in both species following i.v. administration, consistent with the high metabolic stability in rat, rhesus, and human microsomes. ELN-441958 has high oral exposure and moderate plasma half-lives in rats and rhesus monkeys. The oral availability of ELN441958 in rats was 57%. ELN-441958 dose-dependently reduced carrageenan-induced thermal hyperalgesia in a rhesus monkey tail-withdrawal model, with an ED50 3 mg/kg s.c. [1]

SMAD3 is a receptor-regulated intracellular protein that functions downstream of TGF-β and activin receptors and mediates their signaling, playing a role in cell proliferation, differentiation, apoptosis and formation of extracellular matrix. Smad3 Inhibitor, SIS3 is a cell-permeable pyrrolopyridine compound that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling with no effect on Smad2, p38 MAPK, ERK, or PI 3-K signaling. It has been shown to reduce TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.

5-Ethynyluridine (5-EU) is a potent cell-permeable nucleoside can be used to label newly synthesized RNA. 5-Ethynyluridine can be used for isolation and sequencing of nascent RNA from neuronal populations in vivo. 5-Ethynyluridine can be used to identify changes in transcription in vivo in nervous system disease models.

TH1760 is a first-in-class, potent, selective and cell-active NUDT15 (MTH2) inhibitor with an IC50 value of 25 nM.

A novel potent, selective inhibitor of phosphorylation and transcriptional activity of STAT5, but not STAT3, AKT, or Erk1/2 phosphorylation.

A novel selective STAT3 inhibitor that inhibits JAK2-STAT3 activation but has no effects on other transcription factors such as NF-κB, and kinases such as AKT, ERK, and c-Src.

α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer[1].

PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity.

A potent and selective Akt inhibitor with Ki of 0.16 nM for Akt1.

UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2.

S107 is a RyR-selective 1,4-benzothiazepine derivative that stabilizes RyR2 channels by enhancing the binding affinity of calstabin2 to mutant and/or PKA-phosphorylated channels.

BAY2335218(BAY-218) is the first-in-class AhR antagonist for overcoming tumor-mediated immunosuppression.