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.

AD 2900 (AD2900, AD-2900) is a novel potent, broad S1P receptor antagonist with IC50 of 3.8, 3.2, 6.2, 5.9 and 0.405 uM for S1P1, 2, 3, 4 and 5 respectively.

GSK 525762A is a potent small molecule inhibitors that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4).

OTX-015 is a new potent BRD2/3/4 inhibitor with evident anti-proliferative activity in several cell lines representative of mature B-cell tumors.

T5910047 (T-5910047) is a small molecule inhibitor of MyD88-dependent signaling pathways, disrupts MyD88 homodimeric formation; inhibits SEB-induced inhibition of cytokine production in PBMCs with IC50 of 2-10 uM, also inhibits SEA-induced pro-inflammatory cytokine production, shows no toxicity in primary cells up to 100 uM.

CXCR6 inhibitor 81 is a potent (EC50=40 nM) and selective orally bioavailable small molecule antagonist of human CXCR6 receptor; Compound 81 displays >10-fold improvement in potency in both the β-arrestin and cAMP assays (IC50 =40 and 540 nM, respectively) compared to ML339. CXCR6 inhibitor 81 inhibits migration of SK-HEP-1 hepatoma cells in a dose dependent manner. Compound 81 has promising oral DMPK data, significantly decreases tumor growth in a 30-day mouse xenograft model of HCC.

UC-764865 (UC764865) is a small-molecule inhibitor that targeted ubiquitin-conjugating enzyme UBE2N active site.UC-764865 blocks ubiquitination of innate immune- and inflammatory-related substrates in human AML cell lines.Inhibition of UBE2N function disrupted oncogenic immune signaling by promoting cell death of leukemic HSPCs while sparing normal HSPCs in vitro.

A potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively.

BIM-26226, gastrin-releasing peptide, is a potent and selective antagonist of bombesin receptor. BIM-26226 inhibits BN- or GRP-stimulated amylase release with IC50s in the nanomolar range. BIM-26226 can be used for the research of cancer.

Acid-C3-SSPy is a cleavable DBA-DM4 linker used in the synthesis of DBA-DM4, a drug-linker conjugate for ADC.

CEP-11981 is a potent, multi-targeted, orally active, pan-VEGFR, TIE-2 and FGFR1 inhibitor with IC50 of 3-100 nM.

Finasteride Carboxaldehyde is a metabolite of Finasteride in human bile (M2 metabolite).

1-m-PES is an electron mediator which has higher stability of solutions than 1-Methoxy PMS. The stability in neutral to alkali conditions has been extremely improved with 1-Methoxy PES. 1-M-PES is a stable small-molecular compound and it has an equal or higher thermal stability than diaphorase. The 1-Methoxy PES solution can be stored long term.

A viral RNA-dependent RNA polymerase (RdRp) inhibitor that acts as a non-obligate RNA chain terminator.

(-)-Sparteine sulfate pentahydrate is a class 1a antiarrhythmic agent and a sodium channel blocker.

Heparin sodium salt (MW 15kDa) (Sodium heparin (MW 15kDa)) is a polymer of Heparin with the molecular weight of 15kDa. Heparin sodium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin factor IIa and factor Xa.

Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.

DiR is a long-chain carbocyanine dye. Carbocyanine dyes are widely used as Di to label cells, organelles, liposomes, viruses and lipoproteins.

AEBSF HCl is a broad spectrum, irreversible serine protease inhibitor.

L-p-Bromotetramisole is a cell-permeable inhibitor of all four human AP isoenzymes (Kis =18 and 56 μM for PLAP and NSAP, respectively).