Nrf2-Activator is a potent Nrf-2 activator.

Selective RIP3 kinase inhibitor

(E/Z)HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM.

Selnoflast (example 6) is a NLRP3 inhibitor (extracted from patent WO2019008025).

QcrB inhibitor TB47 (TB47) is a novel antimycobacterial agent that fuctions as a putative respiratory complex III (QcrB) inhibitor with MIC of 0.016-0.5 ug/mL against a panel of 56 M. tuberculosis clinical isolates.

MRTX 1133 is a potent and selective KRAS G12D inhibitor. MRTX1133 targets the KRAS G12D protein in both active and inactive states. In preclinical studies, MRTX1133 exhibited a long half-life, an ability to bind the KRAS G12D protein in both active and inactive states, and selective inhibition of KRAS G12D mutant cancer cells.

TACH101 (QC8222, TACH 101) is a reversible, α-ketoglutarate competitive, selective and potent inhibitor of KDM4 isoforms A-D with IC50 values of <0.1 uM against all four isoforms.TACH101 demonstrated potent increase of H3K36me3 levels (EC50 <0.001 uM, HTRF) in KYSE-150 cell line engineered to overexpress KDM4C and showed potent anti-proliferative activity in multiple cell lines in OncoPanel.Sub-micromolar levels of TACH101 induced apoptosis in human colorectal (HT-29), esophageal (KYSE-150), and triple negative breast cancer (MDA-MB-231) cell lines with EC50s of 0.033-0.092 uM.TACH101 triggered effective tumor growth control in xenograft models including colorectal, esophageal, gastric, breast, and lymphoma with tumor growth inhibition of up to 100%.

Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.

SBP-3264 is a valuable chemical probe for understanding the roles of STK3 and STK4 in acute myeloid leukemia (AML).

Dihydroresveratrol is an SIRT1 activator. It is a primary metabolite of resveratrol.

10-Hydroxycanthin-6-one is an antileukemic canthin-6-one alkaloid from Brucea antidysenterica. Antitumor agent.

9-Hydroxycanthin-6-one is an alkaloid compound. 9,10-Dimethoxycanthin-6-one exhibits NF-κB inhibitory effects with an IC50 of 3.8 μM.

9-Methoxycanthin-6-one, a canthin-6-one alkaloid, is present in intact plant parts and in callus tissues of different explants. 9-Methoxycanthin-6-one shows anti-tumor activity.

Canthin-6-one displays a wide range of biological activities, such as antimycobacterial activity.

LOXO-305 is an investigational, novel, selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. LOXO-305 was designed to reversibly bind BTK, preserve activity in the presence of the acquired resistance, and avoid off-target kinases that have complicated the development of both covalent and investigational non-covalent BTK inhibitors.LOXO-305 is a highly selective, non-covalent BTKi that inhibits both wild type (WT) and C481-mutated BTK with equal low nM potency was developed.

AZD5462 is a selective oral allosteric relaxin family peptide receptor 1 (RXFP1) agonist with pEC50 of 7.8. AZD5462 has better kinetic solubility and shows much improved metabolic stability compared to AZ7976 in vitro.

A novel specific glycomimetic E-Selectin antagonist with Kd of 0.46 uM, IC50 of 1.75 uM.

Lipase Substrate is a substrate of lipase to detect activity.

Zevotrelvir (Compound 52) is a coronavirus inhibitor with IC50 ranges of <0.1 μM and <0.1mM for 229E hCoV and SARS-CoV-23C-like (3CL) proteases, respectively. Zevotrelvir has the potential to study viral infections.

PC-766B is a macrolide antibiotic. PC-766B is active against Gram-positive bacteria, and some fungi and yeasts, but inactive against Gram-negative bacteria. PC-766B shows antitumor activity against murine tumor cells. PC-766B has weak inhibitory activity against Na+, K+-ATPase.

NSC89641 inhibits MERS-CoV Mpro, with an IC50 value < 3.5 μM. NSC89641 exhibits the high inhibitory potency against SARS-CoV-2 Mpro enzymatic activity, with an IC50 of 3.05 μM.

Lacutoclax is a Bcl-2 inhibitor with antineoplastic activity.

Votoplam is a gene splicing modulator, used to inhibit Huntington's disease.

Tibremciclib is a CDK4 inhibitor with antineoplastic activity.

SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway.

Igermetostat is EZH2 inhibitor, used in cancer research in vivo and in vitro.

Icalcaprant is a kappa-opioid receptor antagonist.

OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study.

Ancistrotecine B (Compound 2) is a Nav1.7 channel inhibitor (IC50: 0.73 μM). Ancistrotecine B relieves inflammatory pain in mice.

Guvacine hydrobromide, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine hydrobromide inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.