ENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models.

Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of GABAA receptors. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors with IC50 values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.

CMPPE is a GABAB receptor positive allosteric modulator (PAM) that inhibits alcohol self-administration and reinstatement behavior in rats.

Cinazepam is a partial GABAA receptor agonist and a benzodiazepine derivative with anxiolytic and sedative properties. Cinazepam can be utilized in research related to sleep disorders.

Ciclotizolam (WE-973) is a thienotriazolodiazepine with anticonvulsant and anti-aggressive activities. Ciclotizolam binds to benzodiazepine receptors in the central nervous system. Ciclotizolam decreases total sleep time in cats.

3-Hydroxy desalkylflurazepam is a benzodiazepine with potential sedative and anxiolytic effects.

CRAC intermediate 2 is a intermediate compound for CRAC inhibitor synthesis, extracted from patent WO 2013059666A1.

NS3736 is an orally effective chloride channel inhibitor that can be used for the research of osteoporosis. NS3736 targets the CIC-7 channel in osteocytes, blocks osteoclast acidification and resorption in vitro, with IC50=30 μM. In a rat model of ovariectomy-induced osteoporosis, NS3736 can enhance bone strength and bone density.

Allobetulone (N066-0059) is a TMEM16A inhibitor (IC50: 0.24 µM). Allobetulone (N066-0059) can be used in anti-cancer research.

Crinecerfont tosylate (SSR-125543 tosylate) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont tosylate can be used for Classic congenital adrenal hyperplasia (CAH) research. Crinecerfont tosylate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

CFTR corrector 18 (Compound I-99) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. CFTR corrector 18 facilitates the processing and trafficking of CFTR, increasing the number of CFTR on the cell surface. CFTR corrector 18 is promising for research of cystic fibrosis (CF).

O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of the non-selective β-adrenergic receptor (β-AR) antagonist Carvedilol. O-Desmethylcarvedilol inhibits store-overload-induced calcium release in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2R4496C) mutation (IC50 = 7.62 µM). O-Desmethylcarvedilol reduces increases in heart rate and prevents decreases in diastolic blood pressure induced by Isoproterenol in conscious rabbits (ED50s = 32 and 5 µg/kg, respectively).

Niguldipine monohydrochloride is a calcium channel blocker that inhibits P-glycoprotein and can be used in tumor research. Niguldipine monohydrochloride inhibits Cav 3.2, with an IC50 of 0.9 μM.

Hexadecylphosphoserine TFA is a phospholipid molecule that contains a long-chain alkyl (hexadecyl) and a phosphoserine group, giving it a high affinity for the cell membrane. Hexadecylphosphoserine TFA can exert antitumor activity by modulating [Ca++]i and its related signaling pathways, making it useful for research in the field of breast cancer.

Etripamil (MSP-2017) hydrochloride is a short-acting, L-type calcium channel antagonist that can be used in the study of paroxysmal supraventricular tachycardia (PSVT). Etripamil hydrochloride inhibits calcium influx through slow calcium channels, thereby slowing atrioventricular node conduction and prolonging the atrioventricular node refractory period.

dl-Tetrandrine is an orally active and brain-penetrant calcium channel blocker that inhibits voltage-dependent calcium channels. dl-Tetrandrine selectively blocks Ca2+ influx with an IC50 value of approximately 1-10 μM. dl-Tetrandrine exerts anti-inflammatory, immunosuppressive, and anti-arrhythmic activities by inhibiting intracellular calcium overload, and can reverse multidrug resistance in tumor cells. dl-Tetrandrine is promising for research of autoimmune diseases (such as rheumatoid arthritis), cardiovascular diseases, and tumor drug resistance reversal.

CGP 28392 is an activator for calcium channel, and reactivates the oxygen evolution in calcium-deficient photosystem II (PS II) particles.

Cav 3.1 blocker 1 (compound 12) is a T-type calcium channel blocker with an IC50value of 160 nM for Cav3.1. Cav 3.1 blocker 1 weakly inhibits Cav 3.2 (IC50 of 5000 nM), and shows no inhibition on Cav 3.3 and Cav 1.2 (IC50 of >10000 nM).

AK-2-38, a Nifedipine analogue, is a calcium channel antagonist. AK-2-38 also has partial agonist effects on isolated guinea pig left atrium.

Adenophostin A is a potent inositol triphosphate (IP3) receptor agonist, which binds to IP3 receptors with high affinity and effectively stimulates the release of calcium ions (Ca2+).

8-Br-7-CH-cADPR disodium (7-Deaza-8-bromo-cADPR) is a potent cADPR antagonist. 8-Br-7-CH-cADPR disodium shows partial inhibition of calcium elevation caused by sTIR dimerization. 8-Br-7-CH-cADPR disodium significantly decreases Paclitaxel-induced axon degeneration.

(S)-Albuterol is a muscarinic receptor and phospholipase C activator. (S)-Albuterol increases intracellular free calcium in airway smooth muscle.

(2R,3R)-Diltiazem hydrochloride is an isomer of Diltiazem hydrochloride. Diltiazem is an orally active L-type Ca2+ channel blocker. Diltiazem shows antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.

WR-S-462 is a STAT3 inhibitor. WR-S-462 effectively suppresses STAT3 phosphorylation and biological functions in vitro. WR-S-462 inhibits MDA-MB-231 cells with an IC50 of 0.03 μM. WR-S-462 displays a strong binding affinity towards the STAT3 protein with a Kd of 58 nM. WR-S-462 inhibits the nuclear translocation of p-STAT3, selectively inhibits the expression of p-STAT3Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells such as Cyclin D1, Bcl-2, and Bcl-xl. WR-S-462 inhibits TNBC (triple-negative breast cancer) growth and metastasis.

NW16 is an orally active inhibitor for STAT3 with Kd of 11.0 μM. NW16 arrests the cell cycle at S phase, induces apoptosis in HCT116, and inhibits the proliferation of cancer cell HCT116, A549, and B16 with IC50s of 0.28, 1.22, and 9.86 μM, respectively. NW16 induces the production of ROS, inhibits the PI3K/AKT signaling pathway, and thus exhibits antitumor efficacy in mouse model.

VB1080 (compound 12) is a potent PIM inhibitor with IC50 values of 69.5, 4996, 9.88 µM for PIM1, PIM2, PIM3, respectively. VB1080 shows cytotoxicity. VB1080 shows anthelmintic activity.

Golidocitinib 1-hydroxy-2-naphthoate is a derivative of Golidocitinib, an oral, potent, selective inhibitor of Janus kinase 1 (JAK1) with an IC50 of 70 nM. It exhibits enhnaced antitumor activity and can be used for the treatment of cancer, including peripheral T cell lymphoma (PTCL).

(3R,4S)-Tofacitinib is a less active enantiomer of Tofacitinib and a first-in-class inhibitor of JAK3 with an IC50 of 1 nM. It is highly efficacious in treating rheumatoid arthritis (RA).

Milpecitinib (Compound 21a) is a potent, selective Janus tyrosine kinase (JAK) inhibitor with anti-inflammatory activity. Milpecitinib is promising for research of cancers and inflammatory disorders.

LNK01004 is a JAK inhibitor with strong inhibitory effects on JAK1 (IC50: 10 nM), JAK2 (IC50:＜0.51 nM) and TYK2 (IC50: 1.0 nM) . LNK01004 can simultaneously inhibit multiple cytokine-induced p-STAT signaling pathways. LNK01004 can be used in the research of diseases such as atopic dermatitis.