Adenosine receptor antagonist 1 is a A2aR-selective antagonist with an IC50 of 0.29 nM and displays 14-fold more selective for A2aRthan A2bR.
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].
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].
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].
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.
N,N-Dimethylglycine hydrochloride is a Glycine (HY-Y0966) derivative[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.
11-Hydroxyhumantenine is an alkaloid compound isolated from the EtOH extract of the stems of Gelsemium elegans[1].
Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively.
L-Methionine-d3 is the deuterium labeled L-Methionine. L-Methionine is the L-isomer of Methionine, an essential amino acid for human development. Methionine acts as a hepatoprotectant.
Araliadiol is a polyacetylenic compound isolated from the leaves of Aralia cordata Thunb. Araliadiol inhibits MCF-7 cells growth with an IC50 value of 6.41 µg/mL[1].
6-Chloro-L-tryptophan is a Tryptophan derivative. 6-Chloro-L-tryptophan can be used as a substrate for KtzQ[1].
Substance P, [Met-OMet11] is a selective SP-P agonist. Substance P, [Met-OMet11] also is an active peptide. Substance P, [Met-OMet11] can be used for various biochemical studies[1][2].
Hexylgallate (Hexyl 3,4,5-trihydroxybenzoate), a alkyl ester derivative of gallic acid, exhibits potent antimalarial activity against Plasmodium falciparum, with IC50 of 0.11 mM[1].
Tri-p-tolylamine-15N is the deuterium labeled Tri-p-tolylamine[1].
Duoperone is a neuroleptic agent and also a antiemetic agent in animal models.
SCO-PEG7-Maleimide is a cleavable ADC Linker containing 3 PEG units. SCO-PEG7-Maleimide can be used as a copper-free click chemical reagent for catalyst-free click reactions. Its maleimide group (-Maleimide) degrades in aqueous media and has been used in drug delivery studies.
K114, a fluorescent Congo Red analogue, binds tightly to amyloid fibrils with an EC50 of 20-30 nM[1].
Antiarrhythmic agent-1 (example I) is an antiarrhythmic agent and an IKr potassium channel blocker (IC50<1 μM)[1].
S 16474 is an antagonist of Neurokinin-1 Receptor.