DHNA (KIS20) is a PDH kinase 4 (PDK4) inhibitor with an IC50 of 18 μM. DHNA can be used for the study of heart failure.

PX20350 is a FXR agonist with EC50s of 83 and 10 nM for mFXR and hFXR, respectively. PX20350 significantly induces NDRG2 mRNA expression. PX20350 potently reduces liver tumor cells (SK-GI-18 cells) growth and metastasis, and has anti-tumorigenic activity in orthotopic xenograft mouse models.

UR-1505 is a nuclear factor of activated T cells (NF-AT) inhibitor. UR-1505 can suppress CD3/CD28 induced T cell proliferation, increase p27KIP levels, and induce G1/S cell cycle arrest. UR-1505 can also inhibit the production of IL-5 and IFN-γ in activated T cells. UR-1505 has immunomodulatory properties and can be used in the study of atopic dermatitis.

SCYX-6759 is an orally active, blood-brain barrier permeable anti-T. brucei agent. SCYX-6759 inhibits cytochrome P450 (IC50s: 30.3, 30.6, 47.4 μM for 2D6, 2C9, 2C19, respectively.) SCYX-6759 exhibits potent activity against T. b. brucei 427, T. b. rhodesiense STIB900, and T. b. gambiense STIB930, with IC50s of 0.07, 0.038 and 0.030 μg/mL, respectively.

Z169667518 is a ligand of IL-6. Z169667518 can inhibit IL-6-induced STAT3 reporter activity with an IC50 of 2.7 µM. Z169667518 can be used in the research of IL-6-related diseases.

CI-1040 (PD 184352) hydrochloride is an orally active, highly specific inhibitor of MEK, with an IC50 of 17 nM for MEK1.

CTS-21166 is a blood-brain barrier-permeable and orally active BACE1 inhibitor. CTS-21166 reduces brain Aβ levels. CTS-21166 can be used in the research of Alzheimer's disease.

KL1333 hydrochloride is an orally active NAD+ modulator that reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, leading to increased intracellular NAD+ levels through NADH oxidation. Elevated NAD+ levels trigger activation of SIRT1 and AMPK, and subsequently activate PGC-1α. KL1333 hydrochloride improves energy metabolism and mitochondrial dysfunction in mitochondrial encephalomyopathy, lactic acidosis, and stroke-like episodes (MELAS) fibroblasts. KL1333 hydrochloride protects against cisplatin-induced ototoxicity in mouse cochlear cultures.

UC-84 (NSC-615985) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with anti-HIV activity.

RPX 7546 is a potent inhibitor of metallo-𝛽-lactamases (MBLs) with IC50 values of 1.4 and 48 μM for IMP-1 and IMP-78, respectively. RPX 7546 has antibacterial activity.

Ifebemtinib (tosylate) (BI-853520 (tosylate); IN-10018 (tosylate)) is a highly selective PTK2 kinase inhibitor. Ifebemtinib (tosylate) demonstrates anti-tumor activity. Ifebemtinib (tosylate) inhibits FAK autophosphorylation in prostate carcinoma cells. Ifebemtinib (tosylate) can inhibit spheroid formation and orthotopic tumor growth in vivo. Ifebemtinib (tosylate) can be studied in anticancer research such as solid tumors, breast cancer, and malignant pleural mesothelioma.

PSB-1737 is a human-selective GPR17 agonist with an EC50 for human GPR17 of 27 nM, and its activity on murine GPR17 is relatively weak (EC50 > 10 μM). PSB-1737 shows no significant inhibition at the glycine binding site of NMDA receptors, and has no significant agonistic or antagonistic activity on P2Y receptor subtypes. PSB-1737 can be used in demyelinating diseases (such as multiple sclerosis) or inflammatory-related anemia.

Illudinine, a sesquiterpenoid alkaloid, is a monoamine oxidase B (MAO-B) inhibitor with an IC50 of 18.3 μM. Illudinine can be used for research on neurological diseases.

AG-1284 is a HIV proteinase inhibitor with an EC50 of 0.5 mg/mL. AG-1284 can be used for the research of infection.

TY-51924 (ethanol sodium) is a highly selective NHE-1 inhibitor (IC50 = 0.095 μM). TY-51924 (ethanol sodium) can significantly reduce the infarct size and myocardial enzyme release. TY-51924 (ethanol sodium) is commonly used in the study of ischemia-reperfusion injury.

(R,R)-VRT-534 is the (R,R)-enantiomer of VRT-534). VRT-534 (Compound 3) is a chemical chaperone targeting connexin 26 (Cx26). Vrt-534 exhibits dose-responsive binding to recombinant WT Cx26 and mutant Cx26 K188N with EC50s of 19 and 5 μM, respectively. Vrt-534 can be used in research related to hearing impairment.

cBu-Cit-PAB (Compound 13) is a key intermediate of ADC linker. cBu-Cit-PAB can be used for synthesis of antibody-drug conjugates (ADCs).

Ac-BIM-acid bromide is a derivative of Acridine. Ac-BIM-acid bromide significantly inhibits amyloid fibrillation. Ac-BIM-acid bromide modulates the structure of N-terminal region of Saccharomyces cerevisiae Stm1 protein (Stm1_N1-113) and the amyloid morphology of human Aβ42 protein, inhibiting theirs growth. Ac-BIM-acid bromide can be used for Alzheimer’s disease research.

Dioctatin A hydrochloride is a metabolite of Streptomyces and an inhibitor of human dipeptidyl aminopeptidase II. Dioctatin A hydrochloride can inhibit aflatoxin production by Aspergillus parasiticus with an IC50 of 4.0 μM. Dioctatin A hydrochloride can reduce the mRNA levels of aflatoxin biosynthetic genes and the regulatory gene aflR, inhibit conidiation and decrease the mRNA level of the brlA gene, and also promote kojic acid production. In addition, Dioctatin A hydrochloride can inhibit sterigmatocystin production. Dioctatin A hydrochloride has pleiotropic regulatory effects on the production and differentiation of fungal secondary metabolites.

J-104123 is an inhibitor of squalene synthase with monocarboxylic acid structure. J-104123 can lower serum cholesterol level in dog models.

CHIPOpt, a peptide, is an orthosteric CHIP TPR domain inhibitor with a Kd of ∼16 nM. CHIPOpt has anti-aggregation activity and decreases p.tau ubiquitination with little effect on unmodified tau. CHIPOpt can be used for Alzheimer’s disease research.

N-Benzyl-N-demethylpronqodine A (Compound 16) is an inhibitor of NAD(P)H:quinine acceptor oxidoreductase 1 (NQO1) with an IC50 of 83.3 nM.

(Rac)-AAA is the racemate of AAA. (Rac)-AAA is an antagonist of 20-HETE receptor. (Rac)-AAA can increase the expression of GPR75 receptor in androgen-insensitive prostate cancer cells. (Rac)-AAA dose-dependently increases p38 phosphorylation. (Rac)-AAA induces a significant decrease in the phosphor-AKT signal in nuclei of cells. (Rac)-AAA mitigates the NF-κB signal in unstimulated cell nuclei. (Rac)-AAA can diminish the membrane associated signal intensity. (Rac)-AAA decreases the FAK phosphorylation induced by 20-HETE.

KT53 is a highly active, selective, and cell penetrable GSTO1 inhibitor. KT53 can effectively inhibit GSTO1 activity in MDA-MB-435 (IC50 = 35 nM) cells. KT53 significantly enhances the killing effect of cisplatin on MDA-MB-435 cancer cells. KT53 can be used for cancer research.

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HPK1 ligand-Linker Conjugate 1 is a synthesized target protein ligand-linker conjugate that can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-5. PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader with anti-tumor activity.

JMV 3008 is a GHS-R1a antagonist with an IC50 of 5.6 nM. JMV 3008 can be used in the research of diseases such as diabetes and obesity.

BMS 605339 is a linear tetra-peptide α-ketoamide inhibitor of HCV NS3 protease. BMS 605339 can be used in research related to hepatitis C (HCV infection).

RS-0481 is an orally active lymphocyte population function restorer. RS-0481 enhances IL-2 production activity. RS-0481 can re-establish the function of certain lymphoid cell populations impaired by the presence of a growing tumor in an animal. RS-0481 markedly augments the tumor-specific cytotoxic T lymphocytes, TDTH, and the nonspecific lymphokine-activated-killer-cell-like cell responses.

(1S,2S,3R)-PLX-4545 is the (1S,2S,3R) enantiomer of PLX-4545. PLX-4545 is an orally active and selective cereblon-based molecular glue degrader of IKZF2 (zinc finger transcription factor Helios). PLX-4545 can reprogram immunosuppressive regulatory T cells into pro-inflammatory effector T cells, thereby enhancing anti-tumor immune responses.