specificity

BX430 is used for chronic pain and cardiovascular disease and it is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity.

BCI-215 causes selective cancer cell cytotoxicity in part through non-redox-mediated activation of MAPK signaling

GNF4877 is a small molecule inhibitor, a potent dual-specificity kinase inhibitor targeting DYRK1A (IC50=6 nM) and GSK3β (IC50=16 nM). This compound promotes β-cell proliferation by blocking NFATc nuclear export (EC50=0.66 μM for mouse R7T1 cells) and is primarily used for research on β-cell regeneration related to diabetes.

GSK-626616 is a potent and orally bioavailable DYRK3 inhibitor (IC50: 0.7 nM). It inhibits other members of the DYRK family with similar potency. GSK-626616 is a potential therapy for the treatment of anemia.

Harmine (Telepathine) is an alkaloid isolated from seeds of Peganum harmala.

Harmine hydrochloride (telepathine hydrochloride) is extracted from Peganum Harmala Genus.

AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) is a potent and selective Dyrk1B kinase inhibitor with an IC50 of 7 nM.

CLK-IN-T3 is an inhibitor of CLK1, CLK2, and CLK3 with IC50s of 0.67, 15, and 110 nM. CLK-IN-T3 exhibits anti-cancer activity.

ID-8, a DYRK inhibitor, sustains embryonic stem cell self-renewal in long-term culture.

GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.

Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.

AZ191(IC50 of 17 nM) is an effective and specific DYRK1B inhibitor. The specificity of AZ191 for DYRK1B is about 5- and 110-fold greater over DYRK1A and DYRK2, respectively.

LDN-192960 is a potent inhibitor of Haspin and DYRK2 (IC50s: 10 nM and 48 nM).

SR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.

Avelumab is a humanized anti-PD-L1 monoclonal antibody that binds to PD-L1 with high specificity (Kd = 0.1 nM) and exhibits potential antibody-dependent cell-mediated cytotoxicity (ADCC). Avelumab exerts a dual mechanism of action, combining direct antitumor activity with ADCC. Avelumab is used in research on cancers such as Merkel cell carcinoma.

Necrostatin-1 (Nec-1) is a specific RIP1 inhibitor and necrotic apoptosis inhibitor, which inhibits TNF-α-induced necrotic apoptosis and also inhibits IDO.

ML385 is an NRF2 inhibitor (IC50=1.9 μM) with novelty and specificity. ML385 has anti-inflammatory activity by modulating anti-oxidative stress through the inhibition of NRF2. ML385 also exhibits anti-tumor activity.

Disulfiram (TETD) is an inhibitor of the acetaldehyde dehydrogenase ALDH, inhibiting hALDH1 and hALDH2 (IC50=0.15/1.45 μM) with specificity. Disulfiram is acutely sensitized to alcohol and also inhibits GSDMD pore formation.

Gut restricted-7 (GR-7) is a potent, covalent, orally administered, gut-selective bile salt hydrolase (BSH) inhibitor with tissue specificity that localizes to the gut. Gut restricted-7 reduces BSH activity in gut bacteria and decreases levels of unconjugated bile acids in mouse feces, making it suitable for research into metabolism, inflammation, and intestinal diseases.

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

SC79 is an AKT agonist with specificity and blood-brain barrier permeability. SC79 specifically binds to the PH domain of AKT, activates cytoplasmic AKT, and inhibits AKT membrane translocation. SC79 has neuroprotective activity.

Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

JNK-IN-8 (JNK Inhibitor XVI) is an effective JNK inhibitor that inhibits JNK1, JNK2, and JNK3 with IC₅₀ values of 4.7, 18.7, and 1 nM, respectively. JNK-IN-8 offers the advantages of minimal off-target activity, sustained inhibition, and high specificity. JNK-IN-8 primarily acts by blocking the JNK/c-Jun signaling pathway, inhibiting the phosphorylation of the downstream transcription factor c-Jun, thereby regulating the expression of genes associated with inflammatory responses, apoptosis, and stress responses. JNK-IN-8 can be used in research on tumors, inflammation, and neurological diseases.

Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody–drug conjugate that combines the HER2-targeted antitumor specificity of trastuzumab with the potent cytotoxic activity of the microtubule inhibitor DM1, Trastuzumab emtansine enables selective intracellular delivery of the cytotoxic payload to HER2-expressing cells and supporting translational and mechanistic research in advanced breast cancer models.