INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.

NS1652 is a reversible anion conductance inhibitor, blocks chloride channel, with an IC50 of 1.6 μM in human and mouse red blood cells.

EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.

MCHR1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHR1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.

N6F11 is a ferroptosis inducer, and can trigger the degradation of glutathione peroxidase 4 (GPX4) specifically in cancer cells. N6F11 can be used for ferroptosis study.

GAC0003A4 is an LXR inverse agonist that inhibits LXR transcriptional activity. GAC0003A4 also efficiently degrades LXRβ protein. GAC0003A4 has the potential to be used in advanced pancreatic cancer and other refractory malignancies.

c-Kit-IN-3 (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50s of 4 nM, 8 nM for c-KIT wt and c-KIT T670I, respectively. c-Kit-IN-3 displays great potencies against most of the gain-offunction mutations in the juxtamembrane domain, drugresistant mutations in the ATP binding pocket, and activation loops.

BPKDi is a potent bipyridyl PKD inhibitor with IC50s of 1 nM, 9 nM and 1 nM for PKD1, PKD2 and PKD3, respectively. BPKDi blocks signal-dependent phosphorylation and nuclear export of class IIa HDACs in cardiomyocytes.

EGFR-IN-80 (compound 30) is an EGFR inhibitor with a pIC50 of 10.6.

Moclobemide N-Oxide (Ro 12-5637) is N-oxide metabolite of Moclobemide. Moclobemide N-Oxide retains certain MAO-A (monoamine oxidase) inhibitory activity, but is generally present in low concentrations. Moclobemide N-Oxide can be detected by UV absorption at 240 nm.

4-Methyl-4-(pyridin-2-yldisulfanyl)pentanoic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

SPDMV is a glutathione cleavable ADC linker used for the antibody-drug conjugate (ADCs).

AZ13102909 (AZ909) is a potent and selrctive TBK1 inhibitor with IC50 of 5 nM, 100-1000 fold greater for other related kinases.AZ909 combines with AZD6244 to enhance apoptosis in AZD6244-resistant lines in 3D culture.

RXC004 (RXC-004) is a potent, selective Porcupine (PRCN) inhibitor, inhibits functional Wnt production from mouse L-Wnt3a cells with IC50 of 64 pM in luciferase reporters assays.

EN460 is a specific mall molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1), interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation (IC50=1.9 uM).

SCH 529074 is a small molecule mutant p53 reactivator that binds p53 DNA binding domain with Kd of 1-2 uM.

AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM).

LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 with an IC50 less than 2 μM.

Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research.

Merck60 (BRD 6929, Compound-60) is a potent, selective and brain-penetrant inhibitor of HDAC1 and HDAC2 with IC50 of 1 nM and 8 nM respectively.

A potent and selective type III phosphatidylinositol 4-kinase (PI4KIIIβ) inhibitor with IC50 of 3.6 nM.

Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.

URB694 is a carbamate FAAH inhibitor that irreversibly carbamoylate the nucleophile catalytic serine in FAAH active site. URB694 exhibits antidepressant-like activity and cardioprotective effects. URB694 can be used to prepare 11C-Carbonyl-URB694 for in vivo positron emission tomography (PET) imaging studies of the brain FAAH.

PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer.

Nav1.8-IN-8 (Compound A11) is a Nav1.8 channel inhibitor. Nav1.8-IN-8 may prevent associated diseases mediated by sodium ion channels (NaV).

Aspalatone is an anti-platelet aggregator (antithrombotic) that has been shown to prolong bleeding time in the mouse model. Aspalatone generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy.

CSF1R-IN-20 (compound 7a) is a CSF-1R Inhibitor with an IC50 value of 467 nM. CSF1R-IN-20 inhibits CSF-1R auto-phosphorylation.

GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo.