at-130

AT-130 is a HBV virus inhibitor with improved potency (IC50 = 0.13 μM) and reduced toxicity in the HepAD38 cell line. AT-130 blocks HBV replication at the level of viral RNA packaging.

BAT-1306 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. It is applicable for research in colorectal cancer and solid tumors.

BAT-1308 is a human monoclonal antibody targeting PDCD1/PD-1/CD279. It is applicable in the research of cervical cancer and endometrial cancer.

S-Nitrosothiols (RSNOs) are a class of molecules that function as exogenous and endogenous nitric oxide (NO) donors. RSNOs found in vivo include proteins such as S-nitrosohemoglobin and S-nitrosoalbumin, as well as low molecular weight species such as S-nitrosoglutathione (GSNO) and S-nitrosocysteine (CysNO). CAY10565 is a member of a new class of S-nitrosothiol species that act as NO donors under acidic conditions. It decomposes with a half-life of 130 minutes in 0.1 M phosphate buffer, pH 5.0, at 37°C and relaxes phenylephrine-constricted rat aortic strips 71% and 44% at pH 6.0 and 7.4, respectively.

15(R)-Pinane thromboxane A2 is the (R)-epimer of pinane thromboxane A2 . 15(R)-PTA2 does not inhibit collagen-induced platelet aggregation (IC50s = 120-130 μM). It does not affect gastric tone in isolated rat gastric fundus when used at concentrations of 0.5 or 1.5 μg/ml and is less effective than PTA2 at inhibiting prostaglandin-induced contraction of isolated rat stomach muscle.

Streptazolin is a fungal metabolite originally isolated from S. viridochromogenes. It increases NF-κB activity when used at concentrations ranging from 60 to 130 μg/ml, at least in part, via PI3K signaling. Streptazolin enhances TNF-α secretion induced by LPS and enhances IL-8 secretion when used alone or in combination with LPS in THP-1 Blue cells.

Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor, inhibiting binding of substance P by 46% at 100 μg/ml in vitro, and a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. Isolated from Penicillium, it contains an epoxide group at C-19 and C-20, absent in benzomalvins A, B, or E.

PLX647 dihydrochloride is a potent and selective dual inhibitor of FMS and KIT kinases, with IC50 values of 28 nM and 16 nM, respectively. At a concentration of 1 μM, PLX647 dihydrochloride demonstrates superior selectivity against a wide range of 400 kinases, except FLT3 and KDR, where IC50 values are 91 nM and 130 nM, respectively. This orally active compound holds great potential for targeted kinase inhibition.

Zicronapine (Lu 31-130) fumarate, an antipsychotic medication, exhibits potent pro-cognitive effects in animal models and holds promise for treating various neurological and psychiatric conditions. It acts as a strong antagonist at dopamine D1/D2 and serotonin 5-HT2A receptors, highlighting its potential therapeutic efficacy [1] [2].

ZXH-4-130 TFA is a hetero-PROTAC (CRBN-VHL compound) that efficaciously and selectively mediates the degradation of CRBN, achieving approximately 80% degradation at a concentration of 10 nM in MM1.S cells [1].

2'(3')-O-Anthraniloyladenosine-5'-O-triphosphate (2'-ANT-ATP) and its isomer 3'-ANT-ATP are fluorescent derivatives of ATP that spontaneously isomerize. Emitting a maximum light of 428 nm when excited at 330 nm in water, 2'(3')-ANT-ATP specifically inhibits several types of adenylyl cyclase (AC) including mammalian AC1, AC2, and AC5 with inhibition constants (Kis) of 130, 640, and 120 nM, respectively. It also inhibits Bordetella pertussis AC toxin CyaA with Kis of 1.3 µM (in the presence of manganese) and 20 µM (in the presence of magnesium), Bacillus anthracis AC toxin edema factor with Kis of 0.44 µM (with manganese) and 5.15 µM (with magnesium), and Escherichia coli recombinase A (RecA) with a Ki of 6.3 µM.

PGD97 is a selective cyclic peptide inhibitor targeting the CAL/CFTR interaction, with its desulfurization-cyclized form exhibiting a KD value of 6 nM for the CAL PDZ domain. It shows a selectivity of at least 130-fold over the NHERF1/2 PDZ domains. PGD97 stabilizes F508del-CFTR on the cell membrane, enhancing CFTR function necessary for normal pulmonary fluid balance. This compound is applicable in cystic fibrosis research.