mrt-5702D is a molecular glue degrader targeting cereblon (CRBN). mrt-5702D forms a CRBN-MRT-5702D-G3BP2 ternary complex to activate the ubiquitin-proteasome system for G3BP2 degradation. mrt-5702D is promising for research of G3BP2-related cancers (e.g., breast cancer, lung cancer) and neurodegenerative diseases.

Tisolagiline (KDS2010) methylsulfate is the selective, reversible and orally active inhibitor for MAO-B with an IC50 of 8 nM. Tisolagiline methylsulfate exhibits neuroprotective and anti-neuroinflammatory activities.

(R)-ACE-OH is the enantiomer of (S)-ACE-OH.

SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research.

MK-5932 is an orally active, selective, dissociated partial glucocorticoid receptor agonist. MK-5932 inhibits IL-6. MK-5932 induces lymphopenia. MK-5932 restores glucose levels to normal. MK-5932 shows anti-inflammatory effects.

MS-153 is a glutamate transporter activator that can be used as a neuroprotective agent.

PBX-7016 is a Camptothecin derivative. PBX-7016 can selectively inhibit Topoisomerase 1. PBX-7016 can specifically bind and degrade the cancer protein DDX5, thereby down-regulating the expression of anti-apoptotic proteins such as Survivin, Mcl-1, and XIAP, and promoting the apoptosis of cancer cells. PBX-7016 can be used to synthesis of ADCs.

Fmoc-Gly-Thr-OH is an ADC Linker. Fmoc-Gly-Thr-OH can be used to synthesize antibody-drug conjugates (ADCs).

PF 04254644 is an orally active c-Met inhibitor. PF 04254644 inhibits mesenchymal transfer factor/hepatocyte growth factor receptor. PF 04254644 induces myocardial degeneration in rats. PF 04254644 may be used in research on cardiovascular disease and cancer.

RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research.

CT-996 is an orally active GLP-1RA agonist, with an EC50 of 0.49 nM. CT-996 reduces the β-arrestin recruitment and GLP-1R internalization. CT-996 suppresses postprandial blood glucose following a mixed meal tolerance test (MMTT) in mice expressing the human GLP-1 receptor and enhances glucose stimulated insulin secretion (GSIS) during an intravenous glucose challenge in obese monkeys. CT-996 can be used for the study of type 2 diabetes (T2D) and obesity.

Arachidonic acid leelamide, a Leelamine analog, is a pyruvate dehydrogenase kinase (PDK) inhibitor. Arachidonic acid leelamide can be used for the study of breast cancer.

Galeterone (TOK-001) hydrochloride is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research[1][2].

GW273297X is a CYP27A1 inhibitor. GW273297X reduces 27HC concentration in E0771 tumors in APOE3 mice. GW273297X can be used in breast cancer research.

VNPP433-3β (Galeterone 3β-imidazole) dihydrochloride is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β dihydrochloride induces cell apoptosis. VNPP433-3β dihydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β dihydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).

VNPP433-3β (Galeterone 3β-imidazole) hydrochloride is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β hydrochloride induces cell apoptosis. VNPP433-3β hydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β hydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).

25-Azacoprostane (5β-Cholan-24-dimethylamine) is an azasteroid. 25-Azacoprostane has significant inhibitory activity against the molting and metamorphosis processes of various insects. 25-Azacoprostane can be used as insecticide.

FCE 28260 is an orally active 4-azacyclic 5α-reductase (5αR) inhibitor. FCE 28260 exhibits IC₅₀ values for human 5αR type 1 and 5αR type 2 of 36 and 3.3 nM, respectively, and for human and rat prostates with IC₅₀ values of 16 and 15 nM, respectively. FCE 28260 simultaneously blocks the production of dihydrotestosterone (DHT) in the prostate and peripheral tissues. FCE 28260 can significantly inhibit the induction of prostatic and seminal vesicle hyperplasia by testosterone (T) in rat models, without inhibiting the growth of the prostate in DHT implantation models. FCE 28260 can be used for the studies DHT-dependent diseases such as benign prostatic hyperplasia (BPH).

MK-0963 is a steroidal 5α-reductase inhibitor. MK-0963 reduces serum dihydrotestosterone (DHT) concentrations in a dose-dependent manner. MK-0963 can be used for the study of dihydrotestosterone-related diseases such as benign prostate hyperplasia (BPH).

Org 274178-0 is a selective thyroid-stimulating hormone receptor (TSHR) antagonist with a pIC50 value for TSHR is 5.03. Org 274178-0 inhibits the activation of cAMP signaling pathway and phospholipase C (PLC) signaling pathway mediated by thyroid-stimulating hormone (TSH) and TSH receptor-stimulating immunoglobulins (TSIs). Org 274178-0 is promising for research of Graves’ disease and Graves’ ophthalmopathy.

PPI-4955 is a subtype 1 (S1P₁) agonist of sphingosine-1-phosphate receptor with an EC50 of 1.62 nM. PPI-4955-P (the active phosphorylated form) exhibits excellent receptor selectivity and affinity, and the IC50 values for hS1P₁, hS1P₃, hS1P₄, and hS1P₅ are 0.23, 2000, 6.5, and 184 nM respectively. PPI-4955 has significantly improved in vivo phosphorylation efficiency, which can reduce lymphocytes and improve cardiovascular risk. PPI-4955 can be used in immunomodulation research.

NSC-323241 is a potent STT3A-mediated mega protein complex assembly inhibitor. NSC-323241 disrupts he endoplasmic reticulum (ER) mega complex nucleated by STT3A during dengue virus (DENV) and Zika virus (ZIKV) infection. NSC-323241 targets the binding of STT3A subcomplex with viral nonstructural proteins (e.g., NS2B, NS3) and host translocon proteins, disrupting the formation of viral replication microenvironment. NSC-323241 is promising for research of flavivirus infection, such as dengue fever and Zika virus.

iDeg-3 is a selective molecular glue degrader that targets IDO1. iDeg-3 can competitively bind to the heme binding site of apo-IDO1, preventing heme binding and inhibiting the enzymatic reaction that converts tryptophan into kynurenine by IDO1 (IC50 = 46 nM). iDeg-3 can be used for the researches of cancer, infection and neurological disease, such as melanoma.

iDeg-6 is a selective molecular glue degrader that targets IDO1 with a DC50 of 6.5 nM. iDeg-6 can competitively bind to the heme binding site of apo-IDO1, preventing heme binding and inhibiting the enzymatic reaction that converts tryptophan into kynurenine by IDO1 (IC50 = 1.6 μM). iDeg-6 can be used for the researches of cancer, infection and neurological disease, such as melanoma.

Zodasiran is a siRNA targeted to ANGPTL3 in the liver.

Zodasiran sodium is a siRNA targeted to ANGPTL3 in the liver.

XQ-2d sodium is an aptamer that targets TfR/CD71. XQ-2d binds to PL45 cells through recognizing CD71 protein.

Vortosiran, a siRNA, is a blood coagulation factor XI synthesis reducer with anticoagulant activity.

Vortosiran sodium, a siRNA, is a blood coagulation factor XI synthesis reducer with anticoagulant activity.

Volanesorsen scramble negative control is a negative control for volanesorsen) with the sequence: CAUGUTCUTCUGCATGUCAU. Volanesorsen (ISIS 304801) is an antisense oligonucleotide inhibitor of apolipoprotein CIII (apo-CIII) mRNA that can lower triglyceride levels and improve insulin resistance.