family

(Z)-JIB-04 (NSC 693627) is an isomer of JIB-04.

AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.

Aurintricarboxylic acid (NSC-4056) is a strong inhibitor of topoisomerases and other nucleases. It is a potent inhibitor of ribonuclease and topoisomerase II by preventing the binding of the nucleic acid to the enzyme.

Deoxynivalenol (Vomitoxin) is a mycotoxin produced by Fusarium spp. of the single trichothecene family and is commonly found in contaminated food and feed.Deoxynivalenol crosses the intestinal mucosa via a cellular bypass at the tight junctions.Deoxynivalenol transporters are unaffected by inhibitors of P-glycoprotein (PgP) or multidrug resistance-associated protein (MRP). Deoxynivalenol commonly causes diarrhea, vomiting, and gastrointestinal inflammation in humans and animals.

ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM/78.7 nM/197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.

Navitoclax (ABT-263) is a potent oral Bcl-2 inhibitor that binds to Bcl-xL, Bcl-2, and Bcl-w proteins (Ki<1 nM), demonstrating antitumor activity and inducing apoptosis.

Venetoclax (ABT-199) is a Bcl-2 inhibitor (Ki<0.01 nM) with potent, selective, and orally active properties. Venetoclax has a 3-order-of-magnitude lower affinity for Bcl-xL and Bcl-W (Kis=48/245 nM). Venetoclax induces autophagy and apoptosis.

S63845 is a selective myeloid leukemia 1(MCL1) inhibitor that binds to human MCL1 with a Kd of 0.19 nM.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug/mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.

VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.

Zavondemstat (QC8222 free base) is a histone lysine demethylase 4 (KDM4) inhibitor with anticancer and antitumor activity for the study of triple-negative and breast cancers.

Pembrolizumab (MK-3475) is a highly selective humanized monoclonal antibody that antagonizes PD-1. It can block the PD-1 protein on T cells and prevent their interaction with PD-L1 on cancer cells.

3-CPs (3-Carbethoxypsoralen) is a bleomycin-induced serotypic podoplanar polysaccharide in mouse lung fibrosis that belongs to the psoralen family and interferes with antibody-mediated bacterial killing.3-CPs delays bleomycin-induced lung fibrosis in mice and can be used in studies of airway inflammation and asthma.

DDR-TRK-1, a selective discoid domain receptor 1 (DDR1) inhibitor, exhibits an IC50 value of 9.4 nM and also inhibits the TRK family.

TG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).

PF-04447943 (Edelinontrine) is a potent and selective phosphodiesterase 9A inhibitor with an IC50 of 12 nM, which is 78-fold more selective than that used for other PDE family members (IC50>1000 nM).PF-04447943 exhibits anti-inflammatory activity, attenuates inflammatory responses by inhibiting oxidative stress, inflammation, and modulating T-cell polarization, and may be useful for research on sickle cell anemia.

AZ31 is an ATM inhibitor with potency, high selectivity, and oral activity.AZ31 inhibits ATM enzymes, intracellular ATM, with IC50 values of <1.2 nM and 46 nM, respectively.AZ31 exhibits excellent ATR selectivity, PIKK family selectivity, and pan-kinase selectivity.AZ31 is a potent in vitro radiosensitizer that can be used for cancer research.

RMM-46 is a reversible covalent inhibitor with high ligand efficiency and selectivity for MSK/RSK family kinases.

Alpidem (Ananxyl) is an anxiolytic drug from the imidazopyridine family. Alpidem does not produce sedative effects at normal doses, and is instead used specifically for the treatment of anxiety. Alpidem has nanomolar binding affinity for both the central benzodiaze

SU11652 is a potent cell-permeable pyrrole-indolinone compound. SU11652 acts as an ATP-competitive tyrosine kinase receptor and angiogenic inhibitor with greater selectivity for PDGFR-β (PDGFRβ, IC50 = 3 nM), Flk-1 (VEGFR2, IC50 = 27 nM), FGFR1 (IC50= 170

CGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylation of purified Src. CGP77675 exhibits anticancer activity.

LCB 03-0110 Dihydrochloride is a potent inhibitor of the c-Src kinase (IC50 = 1.3 nM) and tyrosine kinases in the BTK and SYK family, as well as in the DDR2 family. It inhibits LPS-induced activation of macrophages and TGF-β1-induced activation of fibroblasts in vitro, inhibits activation of macrophages and fibroblasts, and inhibits scarring in wound healing models.

NHWD-870 is an effective and selective inhibitor of BET family bromodomain only binding to BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. NHWD-870 exhibits potent anti-tumor efficacies and suppresses cancer cell-macrophage interaction through the increase of tumor apoptosis and inhibition of tumor proliferation.

UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 and 85 nM for AXL [1].