Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.

Ligandrol (LGD-4033) is a novel nonsteroidal, oral SARM that binds to androgen receptor with high affinity (Ki of 1 nM) and selectivity.

Ostarine (MK-2866) is a selective androgen receptor modulator (SARMs) that regulates cardiomyocyte function, improves bone healing, regulates uterine function, and influences muscle tissue metabolism.

5-alpha-hydroxy-laxogenin is a derivative of the spirostane-type steroid, laxogenin. 5α-Hydroxy-laxogenin can be used as a plant-based anabolic agent as a dietary supplement.

Src kinase inhibitor I is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes.

AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3.

Phenazopyridine is a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine is a TRPM8 antagonist. Phenazopyridine has a local anesthetic/analgesic effect. Phenazopyridine is used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine can promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases.

(+)-JNJ-37654032 is an orally active and selective androgen receptor modulator. (+)-JNJ-37654032 can be used in the study of muscle-wasting diseases.

5-Chloroisoquinoline (compound 42) is an inhibitor of SARM1 (Sterile alpha and toll/interleukin receptor (TIR) motif containing protein 1), an enzyme involved in axon degeneration that catalyzes multiple activities through a ternary complex mechanism. 5-Chloroisoquinoline can be used in the study of neurodegenerative diseases or axon degeneration.

S23 is a novel Selective Androgen Receptor Modulator(SARM)

ACP-105 is a novel non-steroidal SARM (Selective Androgen Receptor Modulator).

S-40503 is an orally active and selective androgen receptor modulator. S-40503 significantly increases the bone mineral density (BMD) and biomechanical strength of femoral cortical bone.

LG-121071 is an orally active and selective androgen receptor modulator with a Ki of 17 nM.

TFM-4AS-1 is a selective androgen receptor modulator (SARM), and a potent androgen receptor (AR) ligand with an IC50 of 38 nM. TFM-4AS-1 is a gene-selective agonist.

SARM1 Human Pre-designed siRNA Set A contains three designed siRNAs for SARM1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

SARM1-IN-3 (Example 30) is a SARM1 inhibitor. SARM1-IN-3 can be used in the study of chemotherapy induced peripheral neuropathy (CIPN).

SARM1-IN-2 (Example 82) is a SARM1 inhibitor with an IC50 value of <1 μM. SARM1-IN-2 inhibits axonal regrowth, leading to only 6% regrowth after 72 h of exposure. SARM1-IN-2 can be used for the research of axonal degeneration.

LGD 3303 is an androgen receptor agonist.1 It selectively binds to the androgen receptor (Ki = 0.9 nM for the human receptor) over mineralocorticoid, glucocorticoid, and progesterone receptors (Kis = 1,261, 581, and 136 nM, respectively, for the human receptors). It also selectively induces reporter transcription in a reporter assay using CV-1 cells expressing the androgen receptor (EC50 = 3.6 nM) over CV-1 cells expressing the mineralocorticoid or progesterone receptors (EC50s = 3,695 and 2,233 nM, respectively). LGD 3303 (3 mg/kg per day) increases levator ani muscle mass, but not prostate muscle mass, in orchiectomized (ORDX) male rats. It increases body weight and gastrocnemius mass, bone mineral content and density in the lumbar spine and mid-femur, and bone formation rate in ovariectomized (OVX) female rats when administered at a dose of 3 mg/kg per day. LGD 3303 (30 mg/kg per day) increases the time spent in the male area in a sexual preference test by sexually experienced, but not sexually inexperienced, estradiol benzoate- and progesterone-primed OVX female rats.

MK-3984 is a selective androgen receptor modulator (SARM). MK-3984 can be used for the research of muscle wasting associated with cancer.

CMP05 (Endosomolytic compound CMP05) is a novel endosomolytic small-molecule compound that exhibits higher transfection efficiency/ability to induce endosomal escape of oligonucleotides (ONs) than current compounds such as chloroquine.

Topical nonsteroidal antiandrogen (NSAA)

YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of?YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM).

Ezeprogind (AZP-2006) is an orally active neurotrophic inducer. Ezeprogind targets all causes of neurodegeneration and is not only aiming at markers such as Abeta protein or tau protein. Ezeprogind is a potent neuroprotectant and can be used for the research of neurological disorders, including progressive supranuclear palsy (PSP), tauopathies, alzheimer’s and parkinson’s diseases, et al.

GABA-A modulator, blocking the sedative effects without lowering the convulsion threshold

HTT-D3 is a potent, CNS-penetrant, orally bioavailable huntingtin (HTT) splicing modulator, affects HTT pre-mRNA splicing and reduces HTT expression with IC50 of 8 nM.Oral administration of HTT-D3 resulted in dose-dependent and approximately equivalent mHTT protein lowering in both brain and peripheral tissues in mouse models carrying human mHTT transgene, BACHD and Hu97/18.HTT-D3 (10 mg/kg) reduced mHTT mRNA and protein levels in BACHD brain in BACHD mice.

Benznidazole (Ro 07-1051) is an antiparasitic medication, with an IC50 of 20.35 μM for Colombian T. cruzi strains, and has been used in the treatment of Chagas disease.

CO23 is a selective thyroid hormone receptor (TR) α agonist and used for growth and development regulation. CO23 was able to be transported through the blood-brain barrier. CO23 (ip; 0.04-5.0 nmol/g) has ≈50% cholesterol reduction with 0.8 nmol/g dose and higher doses are equally effective. CO23 has no effect at the lowest dose of 0.04 nmol/g and increases Dio1 mRNA 5-, 10-, and 15-fold at the doses of 0.8, 2.5, and 5 nmol/g, respectively.

ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP). It exhibits an EC50 of 1.37 μM for α-casein hydrolysis by HsClpP. ZK53 treatment allosterically activates HsClpP to uncontrollably degrade the essential mitochondrial proteins and is inactive toward bacterial ClpP proteins.

CMP-5 HClis a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 dihydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.