EXP-7711 is a non peptide angiotensin II (Ang II) AT1 receptor antagonist. EXP-7711’s affinity for wild-type AT1 receptor (Ki =180 nM) is lower than peptide antagonists, but higher than losartan (Ki = 12 nM). EXP-7711 can be used for research on cardiovascular conditions.

CR 3834 is a angiotensin-AT1 antagonist. CR 3834 can be used for the research of cardiovascular disease.

Carbaprostacyclin-biotin (cPGI-biotin; Carbacyclin-biotin) is a biotin-bound Carbacyclin (Carbaprostacyclin)). Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.

Jacaric acid methyl ester is a methyl ester form of the conjugated PUFA jacaric acid. Jacaric acid can induce apoptosis selectively in human prostate cancer cells. Jacaric acid induces concentration- and time-dependent LNCaP cell death. Jacaric acid methyl ester can be studied in anticancer research.

8(9)-EET is a major cytochrome P450 (CYP450) metabolite in the renal cortex[1][2]. It activates PPARα in HEK293 cells when used at a concentration of 1 μM but inhibits NF-κB activity induced by IL-1β in a PPARα-dependent and -independent fashion. It is also a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM .

(±)5(6)-EET Ethanolamide is a metabolite of Anandamide generated via oxidation by cytochrome P450 enzymes. (±)5(6)-EET Ethanolamide is also a selective cannabinoid receptor 2 (CB2) agonist. (±)5(6)-EET Ethanolamide has Ki values of 11.4 μM and 8.9 nM for human CB1 and CB2, respectively . (±)5(6)-EET Ethanolamide can be used in research on immunomodulation and neuroinflammation.

KIT-13 is an orally active plasmalogen derivative to inhibit neuroinflammation and mitochondrial DNA leakage associated with Mecp2 deficiency. KIT-13 significantly reduce neurological symptoms and improves the life span of the Rett Syndrome (RTT) model mice. KIT-13 can be used for the study of RTT and other neuroinflammation-related diseases.

KI-ARv-03 is a potent and selective ATP-competitive CDK9 inhibitor with an IC₅₀ of 0.15 μM (at 45 μM ATP), exhibiting over 130-fold selectivity against other CDKs (including CDK1-7). KI-ARv-03 reduces androgen receptor (AR)-driven transcription and proliferation in prostate cancer cells. KI-ARv-03 can be used for leukemia, pancreatic cancer, alveolar rhabdomyosarcoma (ARMS) and castration-resistant prostate cancer (CRPC) research. KI-ARv-03 is a ligand for target protein for PROTAC. KI-ARv-03 can be used to synthesize PROTAC KI-CDK9d-32.

Menin-MLL inhibitor MI-2 dihydrochloride is a competitive and selective Menin-MLL interaction inhibitor with an IC50 value of 446 nM and a Ki value of 158 nM. Menin-MLL inhibitor MI-2 dihydrochloride downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 dihydrochloride is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL).

KUNB106 is a selective Hsp90β inhibitor with KDs of 91 nM and 38 μM against Hsp90β and Hsp90α. KUNB106 exhibits antiproliferative activity against MDA-MB-231 cells, A549 and SKOV-3 cells. KUNB106 can be used for the study of triple negative breast cancer.

Topobexin (Topobexin 9) is a highly selective inhibitor for TOP2B. Topobexin selectively inhibits TOP2B in vitro and immobilizes TOP2B on DNA. Topobexin demonstrates significant protection of cardiomyocytes against DAU-induced damage. Topobexin prevents anthracycline-induced cardiotoxicity and DAU-induced decrease in LV systolic function in vivo with rabbit model.

BB-3497 is a potent, orally active and selective peptide deformylase (PDF) inhibitor. BB-3497 is highly selective for PDF (IC50 = 7 nM for E. coli PDF.Ni) over the other mammalian metalloenzymes (MMP-1/2/3/7 and enkephalinase). BB-3497 exhibits potent activity against gram-positive bacteria and some gram-negative pathogens. BB-3497 protects mice from infection in systemic models of Staphylococeus aureus. BB-3497 can be used for anti-bacterial infection research.

P2Y12R ligand-1 (Compound 41) is a high-affinity P2Y12R ligand with a Ki value of 17.1 nM. P2Y12R ligand-1 labeled with [18F] can be used in studies of brain PET imaging.

MRS8454 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR). MRS8454 can significantly enhance the maximum effect of the standard agonist Cl-IB-MECA by approximately 286%-300%, and significantly reduce its EC50 value. MRS8454 effectively enhances the ability of A3AR agonists to inhibit the cAMP accumulation induced by Forskolin. MRS8454 can be used for the development of molecular probes.

E-2508 free base is an orally active and highly selective corticotropin-releasing factor type 1 receptor (CRF1) antagonist with anxiolytic effects (IC50=11 nM). E-2508 free base blocks CRF-induced cAMP accumulation via CRF1 receptor inhibition. E-2508 free base is promising for research of stress-related psychiatric disorders, such as anxiety and depression.

R-836 is a phosphodiesterase inhibitor. R-836 is a bronchodilator. R-836 can alleviate bronchial constriction caused by antigens or platelet activating factors.

YM-358 hydrate (potassium) is an orally active angiotensin II type 1 (AT1)-receptor antagonist. YM-358 hydrate (potassium) can decrease cardiac volume overload. YM-358 hydrate (potassium) can be used for the research of cardiovascular disease, such as hypertension.

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.