DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway[1].
Corymbosin is a glucoside. Corymbosin can be isolated from the aerial parts of Ballota glandulosissima. Corymbosin also has antifungal flavonoid activity[1][2].
Tretazicar (CB 1954), an antitumor prodrug, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1)[1][2].
Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.IC50 value:Target: β1 receptor
KRAS G12C inhibitor 61 (Example 3) inhibits phospho-ERK 1/2 in MIA PaCa-2 cells with an IC50 value of 9 nM. KRAS G12C inhibitor 61 can be used for research of pancreatic, colorectal, and lung cancers[1].
Glyoxalase I inhibitor 4 (compound 14) is a potent glyoxalase I inhibitor with an Ki of 10 nM[1].
(2R,4S)-H-D-Pro(4-N3)-OH is a click chemistry reagent containing an azide group[1].
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
Superoxide dismutase (SOD) is the only antioxidant enzyme that scavenges the superoxide anion by converting this free radical to oxygen and hydrogen peroxide, thus preventing peroxynitrite production and further damage. Superoxide dismutase is extensively researched and used in anti-inflammatory, antitumor, radiation protection, and antisenility applications[1].
2,3,5,6-Tetrachloroaniline-d3 is the deuterium labeled 2,3,5,6-Tetrachloroaniline[1].
2’-C-β-Methyl-4-deoxyuridine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research[1].
Ethyl linoleate-13C18 (Linoleic Acid-13C18 ethyl ester) is the 13C labeled Ethyl linoleate. Ethyl linoleate inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators[1].
DHODH-IN-12 (Compound 12b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pKa of 5.07[1].
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
5-Phenylcytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
Ciraparantag is a thrombin and factor Xa inhibitors as well as to heparin-based anticoagulants through non-covalent hydrogen bonding and charge interactions. It is reported to antagonize the effects of all coagulants except VKAs and agratroban. [1][2]
6-(3-Methoxyphenyl)-4-methyl-2-(2-morpholinoethyl)pyridazin-3(2H)-one hydrochloride is a methionine adenosyltransferase 2A (MAT2A) inhibitor.
SAH-EZH2 is an EZH2/EPP interaction inhibitor (Kd = 320 nM). SAH-EZH2 suppresses EZH2 expression and H3K27 trimethylation by PCR2 complex. SAH-EZH2 arrests proliferation and induces monocyte to macrophage differentiation of MLL-AF9 leukemia cell line.
IQ-1 is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1 has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
H-Leu-Asp-OH is a biologically active peptide.
AP-C4 is an inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 5.2. AP-C3 does not inhibit cGKII-dependent anion secretion[1].
The compound inhibits TRPC proteins, and more specifically inhibits the TRPC6 protein.
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation[1].
CNV1014802(GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.IC50 value: Target: sodium channel blockerLike lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning produced by PCP, thus confirming their potential in the treatment of cognitive symptoms of schizophrenia. However, higher doses than those required for anticonvulsant efficacy of the drugs were needed for activity in the reversal-learning model, suggesting a lower therapeutic window relative to mechanism-dependent central side effects for this indication. CNV1014802 received orphan-drug designation from the US Food and Drug Administration in July 2013.
N,N-Dimethylglycine hydrochloride is a Glycine (HY-Y0966) derivative[1].
Benzyl-PEG5-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Monomethyl auristatin E intermediate-13 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs)[1].
SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580. IC50 value: 44 nM ( p38α)Target: p38 MAPKSB 239063 reduces inflammatory cytokine production and is neuroprotective following oral administration in vivo.
Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.