Dnp-PLALWAR is a fluorogenic substrate for matrix metalloproteinase-1 (MMP-1) and MMP-8.

GAPDS is a small molecule that targets the glycolytic enzyme glyceraldehyde 3-phosphate dehydrogenase (GAPDH).

Talazoparib, also known as BMN-673 and MDV-3800, is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity (PARP1 IC50 = 0.57 nmol/L). Talazoparib acts as an inhibitor of poly ADP ribose polymerase(PARP) which aids in single strand DNA repair. Cells that have BRCA1/2 mutations are susceptible to the cytotoxic effects of PARP inhibitors because of an accumulation of DNA damage. Talazoparib is theorized to have a higher potency than olaparib due to the additional mechanism of action called PARP trapping. PARP trapping is the mechanism of action where the PARP molecule is trapped on the DNA, which interferes with the cells ability to replicate. Talazoparib is found to be ~100 fold more efficient in PARP trapping than olaparib.

DHAPC is a phospholipid that is very sensitive to oxidation.

Bicyclopyrone is an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (Hpd).

aTAG 2139 (CFT-2139) is an aTAG-based MTH1 fusion protein degrader with a DC50 value of 1.1 nM. aTAG 2139 has a Ki value of 2.1 nM for MTH1.

aTAG 4531 (CFT-4531) is a potent, selective, and onmechanism tool degrader of MTH1 with DC50 value of 0.28 nM and Ki value of 1.8 nM. degradation activity is due to the intricate formation of the ternary complex between the MTH1 aTAG, CRBN E3 ligase, and aTAG tool degrader .

Epalrestat is an orally active aldose reductase inhibitor that acts on diabetic neuropathy.

CDDD11-8 is a potent CDK9 inhibitor co-targeting FLT3-ITD with Ki values of 8 and 13 nM, respectively.CDDD11-8 displays excellent kinome selectivity in a panel of 369 human kinases.CDDD11-8 displays antiproliferative activity against leukemia cell lines, and particularly potent effects against MV4-11 and MOLM-13 cells, which are known to harbor the FLT3-ITD mutation and mixed lineage leukemia (MLL) fusion proteins.CDDD11-8 causes a robust tumor growth inhibition by oral administration in animal xenografts, induces tumor regression at dose of 125 mg/kg.

IL-17 modulator 3 is an IL-17 modulator (US20200247785A1). IL-17 modulator 3 can be used for the research of inflammation, cancer and autoimmune diseases.

Compound 181 is a selective and highly potent stabilizer of the 14-3-3σ/ERα complex. Compound 181 shows potency comparable to the natural product Fusicoccin-A.

BAY2666605 is a potent, small molecule PDE3A-SLFN12 complex inducer with EC50 of 7 nM.BAY2666605 triggers the formation of a complex of two proteins called SLFN12 and PDE3A. This complex drive cancer cells into cell death by a mechanism called apoptosis.

CFT-8634 (CFT8634) is a potent, selective, orally bioavailable BRD9 BiDAC degrader with DC50 of 3 nM, high selectivity over BRD4 abd BRD7.Unlike BRD9 inhibition, BRD9 degradation is efficacious in preclinical models of synovial sarcoma and CFT8634 is ongoing for the treatment of SMARCB1-perturbed cancers.

PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM for human TRPA1.

Novel selective inhibitor of RARγ

Epothilone B is a Taxol-like microtubule-stabilizing agent with EC0.01 of 1.8 μM.

Potent and selective inhibitor of NLRP3, reducing interleukin-1β (IL-1β) production in vivo and attenuating the severity of experimental autoimmune encephalomyelitis (EAE)

IBG4 is a PROTAC-like degrader. IBG4 shows high specificity for BRD4 and does not efficiently degrade BRD2.

IBG1 is a PROTAC-like degrader, which comprises JQ1 tethered to E7820. IBG1 selectively degraded BRD2 and BRD4 but not BRD3. IBG1 results in potent BRD4 degradation with DC50 of 0.15 nM and pronounces growth inhibition in various cancer cell lines.