HTS05585 (Compound Hit-1) is a selective macrophage migration inhibitory factor (MIF) inhibitor with a Kd value of 0.29 μM measured by microscale thermophoresis (MST) and 0.32±0.01 μM verified by isothermal titration calorimetry (ITC). HTS05585 inhibits the release of pro-inflammatory factors (TNF-α, IL-6, IL-1β) from LPS-induced macrophages. HTS05585 is promising for research of inflammation-related diseases such as sepsis.

AH001 is a orally active RhoA inhibitor, which binds a cryptic pocket proximate to GDP within RhoA with a KD of 73.16 nM. AH001 interacts with GDP, stabilizing RhoA’s interaction with its endogenous inhibitor, RhoGDIα. AH001 reduces the downstream MRTFA nuclear translocation and downregulates fibrosis/hypertrophy proteins. AH001 mitigates myocardial remodeling in multiple HF animal models, and in the 3D myocardial tissue model. AH001 exerts its cardioprotective effects through the RhoA-RhoGDIα axis, effectively inhibiting downstream RhoA activation signaling.

KCL-HO-1i is an orally active heme oxygenase-1 (HO-1) inhibitor (rat HO-1: IC50 = 123 nM) and human HO-1: IC50 = 128 nM). KCL-HO-1i targets immunosuppressive LYVE-1+ perivascular tumor-associated macrophages (PvTAMs) in the tumor microenvironment (TME), reduces PvTAM-mediated immune exclusion. KCL-HO-1i demonstrates synergistic anti-tumor efficacy with chemotherapy in MMTV-PyMT spontaneous breast cancer mice or C57Bl/6 mice bearing subcutaneous MN-MCA1 sarcomas. KCL-HO-1i can be used for the study of cancer.

RET ligand-5 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC RET Degrader 1. PROTAC RET Degrader 1 is a potent RET PROTAC degrader with anti-tumor activity.

BL-2401 is an orally active enkephalinase inhibitor. BL-2401 exhibit antinociceptive and antidepressant-like activitiesin association with endogenous opioid systems. BL-2401 can be used for the research of neurological disease.

Thalidomide-OCH2-amide-PEG2-C2-Boc is an E3 ligase ligand-linker conjugate containing a cereblon (CRBN) ligand for E3 ubiquitin ligase and a linker. Thalidomide-OCH2-amide-PEG2-C2-Boc can be used to synthesize PROTAC CDK4/6/9 degrader 2.

MB-11362 is an orally active, selective HCV NS5B polymerase inhibitor and 4′-azidouridine triphosphate prodrug. MB-11362 can be converted to 4′-azidouridine triphosphate after oral administration. MB-11362 can be used in the research of HCV infection.

SRI-45949 is an allosteric modulator of the HIV-DAT-Tat interaction. SRI-45949 has IC50 values of 9.56 μM and 9.34 μM for [3H]DA uptake and [3H]WIN35,428 binding, respectively. SRI-45949 can be used in research related to HIV-associated neurocognitive disorders.

Tezampanel etibutil is an orally active AMPA/GluR antagonist. Tezampanel etibutil can be used in the research of pain, migraine, and neurological disorders.

AC-340 is a potent hybrid VDR agonist/HDAC inhibitor. AC-340 superinduces VDR target genes (e.g., CYP24A1) and inhibits HDAC6 (IC50 = 0.37 μM) with ~10-fold selectivity over HDAC2. AC-340 induces VDR hyperagonism by causing widespread protein hyperacetylation (e.g., tubulin and H3K9/K27), which leads to elevated H3K27 acetylation on VDR target genes. AC-340 can be used for melanoma cancer research.

KB-0742 hydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 hydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 hydrochloride has potent anti-tumor activity.

XSJ110 is a potent irreversible topoisomerase I (Topo I) inhibitor with an IC50 value of 0.133 μM. XSJ110 blocks DNA topoisomerization, induces DNA double-strand breaks, and triggers cell cycle arrest at G0/G1 phase, inducing tumor cell apoptosis. XSJ110 is promising for research of ampullary carcinoma (AC).

SCL-1 is an orally active anti-PD-1/PD-L1 inhibitor. SCL-1 can inhibit PD-1/PD-L1 binding. SCL-1 increases T cells, B cells and natural killer cells. SCL-1 exerts strong tumor growth inhibitory effects that were mediated by effector T-cell induction inside tumors and the up-regulated expression of long non-coding RNAs as neoantigens leading to cytotoxic T lymphocyte activation. SCL-1 can be used for the research of cancer, such as triple-negative breast cancer.

Huib32 is a potent small-molecule inhibitor of USP32 (IC50 = 21.2 nM), exhibiting high selectivity over other closely related deubiquitinating enzymes (DUBs), such as USP8/10/16, UCHL1 and OTUB2. Huib32 reversibly inhibits USP32 by covalently binding to the active site Cys743, which enhances substrate ubiquitination, alters endosomal morphology, and mimics USP32 depletion. Huib32 can be used for breast, ovarian, and lung cancer and Alzheimer's and Parkinson’s diseases research.

BMS-561388 (benzenesulfonate) is a corticotropin-releasing factor receptor (CRFR) antagonist. BMS-561388 (benzenesulfonate) can be used for the research of neurological disease, such as anxiety and depression.

MG-Lin1 is a molecular glucose degrading agent that targets the Lin28 protein. MG-Lin1 can significantly reduce the mRNA levels of let-7 targeting oncogenes. MG-Lin1 can significantly inhibit the migration ability of cancer cells. MG-Lin1 has no obvious cytotoxicity. MG-Lin1 can be used for cancer research.

Lin28 degrader MG-Lin2 is a molecular glucose degrading agent that targets the Lin28 protein. Lin28 degrader MG-Lin2 significantly inhibit the migration ability of cancer cells. Lin28 degrader MG-Lin2 has no significant cytotoxicity. Lin28 degrader MG-Lin2 can be used for cancer research.

JQ-1-Azidopropylamine is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 and a PROTAC linker, which recruits E3 ligases. JQ-1-Azidopropylamine can be used for synthesis of PROTAC JY-21

VU6008055 is a potent, selective, cross the blood-brain barrier and orally actively M4 positive allosteric modulator with EC50 values of 73.4, 19.5 nM for hM4, rM4, respectively. VU6008055 shows antipsychotic-like activity.

Iptriazopyrid (NC-656) is an azole carboxamide herbicide targeting 4-hydroxyphenylpyruvate dioxygenase (HPPD) with a Ki value of 24.3 nM for Arabidopsis HPPD and 33.3 nM for rice HPPD. Iptriazopyrid blocks plastoquinone and carotenoid synthesis, leading to weed chlorosis and death. Iptriazopyrid is promising for research of controlling weeds such as Echinochloa crus-galli in paddy fields.

XL-3156 is a potent, selective, and cross-species cGAS inhibitor. XL-3156 can simultaneously occupy both allosteric and orthosteric sites, and inhibit the interaction and phase separation between cGAS and DNA by stabilizing the closed conformation of the activation loop. XL-3156 can be used in the research of autoimmune diseases, inflammatory conditions and other diseases.

DMP 904 is a noncompetitive full corticotropin-releasing factor receptor (CRFR) antagonist. DMP 904 can inhibit CRF-stimulated adenylate cyclase activity and ACTH release. DMP 904 exhibits anti-depressant and anti-anxiety activity.

EVT-101 free base is a GluN2B antagonist. EVT-101 free base binds at the same GluN1/GluN2B dimer interface as Ifenprodil. EVT-101 free base inhibits calcium influx in chicken-derived cells, with an EC50 of 22 nM. EVT-101 can be used in the research of brain disorders.

NGD 98-2 hydrochloride is an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist

GSK-958108 is a highly selective 5-HT1A receptor antagonist. GSK-958108 is commonly used in the study of neurological conditions.

JNJ-78911118 is a potent, brain-penetrant, selective GluN2A antagonist (IC50 = 44 nM). JNJ-78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. JNJ-78911118 functions as a negative allosteric modulator (NAM) by insurmountably suppressing glutamate efficacy and reducing glycine potency at GluN1/2A receptors. JNJ-78911118 produces profound pharmacodynamic effects in vivo. JNJ-78911118 can be used for depression research.

SJL2-1 is a PRMT5 inhibitor, with an IC50 of 1.56 μM. SJL2-1 suppresses proliferation, migration, and invasion in prostate cancer cells. SJL2-1 promotes apoptosis and blocks the cell cycle at the G0/G1 phase. SJL2-1 can target the binding of PRMT5 in cells and inhibit the methylation and expression of the androgen receptor. SJL2-1 can be used for the study of early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC).

MolPort-002-705-878 is a highly selective FMS-like tyrosine kinase 3 (FLT3) inhibitor with a binding affinity of −11.33 kcal/mol. MolPort-002-705-878 inhibits the proliferation of FLT3-mutated acute myeloid leukemia (AML) cells. MolPort-002-705-878 is promising for research of FLT3-mutated AML.

NP3-742 is an orally active NLRP3 inhibitor that binds to the NLRP3 NACHT domain. NP3-742 inhibits IL-1β release with IC50s of 6 nM and 47 nM in both the cellular and whole blood assays, respectively. NP3-742 is highly selective against a panel of more than 50 enzymes, receptors and sodium and calcium channels. NP3-742 can be used for the study of gout, cardiovascular disease or osteoarthritis.

MCI-225 (DDP-225) hydrate hydrochloride is a selective and orally active noradrenaline (NA) reuptake inhibitor with 5-HT3 receptor antagonism. MCI-225 hydrate hydrochloride has antidepressant-like and anxiolytic-like properties. MCI-225 hydrate hydrochloride can be used for the study of anxiety disorder.