Tirabrutinib hydrochloride (GS-4059 (hydrochloride)) is a selective and novelBTK with IC50 2.2 nm inhibitor.

Rituximab (anti-CD20) is a chimeric anti-CD20 mAb that binds the CD20 antigen on B cells with a binding affinity of 5 nM.

Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic ferroptosis.

Belvarafenib is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.

Cbl-b-IN-3 is a potent proto-oncogene-B (CPL-B) inhibitor of casitas B-series lymphoma (ic50 < 1 nM). Cpl-b, a cyclic E3 ubiquitin protein ligase, is involved in the setting of T lymphocyte activation thresholds. Cpl-b negatively regulates p85 in an independent proteolytic manner, and participates in the recruitment of p85 to CD28 and T cell antigen receptor ζ through its E3 ubiquitin ligase activity. Inhibition of PI3K inhibits the enhancement of Cblb-/ -T cell activation.

Iptacopan (LNP023) is an inhibitor with high affinity for factor B.

PLX-4720 is a potent and selective inhibitor of B-Raf (V600E) (IC50: 13 nM), equally potent to c-Raf-1(Y340D and Y341D mutations).

Dabrafenib (GSK2118436A) is a Raf inhibitor that inhibits C-Raf and B-RafV600E (IC50=5/0.6 nM) and is ATP-competitive. Dabrafenib exhibits antitumor activity for the treatment of B-RafV600E-mutated melanoma.

β-nicotinamide mononucleotide is a product of the nicotinamide-phosphate ribosyltransferase (NAMPT) reaction. β-nicotinamide mononucleotide's actions include its role in cellular biochemical function, cardioprotection, diabetes, obesity-related complications, and Alzheimer's disease.

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

Safinamide mesylate (EMD 1195686 mesylate) , a mesylate salt of Safinamide, can reversibly and specifically inhibit MAO-B (IC50: 98 nM), has 5918-fold selectivity against MAO-A.

TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.

Cyclotraxin B acetate is an antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic properties in mice.

BMS-903452 is a potent and selective GPR119 agonist with EC50 of 14 nM. BMS-903452 is indicated for the treatment of acute and chronic rodent diabetes. GPR119 was mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. GPR119 had no significant inhibitory effect on 9 different cytochrome P450 enzymes (IC50 > 40 μM), did not activate PXR (EC50>50 μM), and was not toxic to liver (HEPG2) cell lines.

Orexin B, rat, mouse Acetate (Rat orexin B) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.

Moiramide B is a potent acetyl coenzyme A carboxylase (ACC) inhibitor (IC50:6 nM) with antimicrobial activity, strongly inhibiting Gram-positive bacteria but weakly inhibiting Gram-negative bacteria.

Givinostat hydrochloride (ITF2357 hydrochloride) is an inhibitor of HDAC with IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride exhibits anti-inflammatory, anti-angiogenic, and antineoplastic activities.

Hemokinin 1 (human) acetate is an endogenous substance P homolog that is a selective agonist at the tachykinin NK1 receptor (IC50 values are 1.8, 370 and 480 nM for NK1, NK3 and NK2 receptors respectively). Has proliferative and antiapoptotic actions on B

SP-146 is a selective, potent and non-ATP-competitive Aurora B inhibitor(IC50 : 0.316 nM).

PSB-1434 is a selective and competitive monoamine oxidase B inhibitor.

MK-0674 is an orally available, selective and potent cathepsin K inhibitor (IC50: 0.4 nM) that inhibits Cat B, Cat F, Cat L, and Cat S. It can be used in metabolism-related diseases.

PSB-1491 is a selective and competitive monoamine oxidase B inhibitor with IC50 of 0.386 nM, >25000-fold selective versus MAO-A.

PI3Kδ-IN-3 (TC KHNS 11) is a PI3Kδ inhibitor with an IC50 value of 9 nM.PI3Kδ-IN-3 has a favorable pharmacokinetic profile and inhibits B cell function.

B-Raf IN 13 is a potent B-Raf inhibitor with anticancer activity.B-Raf IN 13 has an IC50 of 3.55 nM in the BRAF V600E enzyme assay.

BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK/PTK6), displaying an IC50 of 30 nM. Additionally, it effectively suppresses p-SAM68 with an IC50 value of 52 nM. This compound, BRK inhibitor P21d hydrochloride, serves as a valuable tool for evaluating the efficacy of BRK inhibitors in xenograft breast tumor models, enabling the assessment of their in vivo activity.

(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor targeting calpain I (μ-calpain) with a Ki value of 19 nM. It exhibits lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). This compound is potentially useful for investigating calpains' involvement in various processes such as neutrophil chemotaxis, neuronal signaling, and cardiac responses to injury [1].

B I09, an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells.

LY3295668 (AK-01) is a selective inhibitor of Aurora A with Kis of 0.8 nM and 1038 nM for Aurora A and B, respectively.

K777 is a potent, orally active and irreversible inhibitor of cysteine protease. K777 is a potent CYP3A4 inhibitor (IC50= 60 nM). K777 is also a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, which is the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 targets cathepsin-mediated cell entry and wxibits a broad-spectrum antiviral activity. K777 inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

BTK inhibitor 1 (Compound 27) is a BTK inhibitor (IC50: 0.11 nM) with an inhibitory effect on B-cell activation in hWB with an IC50 of 2 nM.

5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20 and 25 nM).

BSH-IN-1 is a potent and covalent inhibitor of gut bacterial recombinant bile salt hydrolases (BSHs; IC50s: 108 nM and 427 nM for B. longum BSH and B. theta BSH).

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

QL-X-138 is a potent and selective BTK and MNK dual kinase inhibitor that binds covalently to BTK and non-covalently to MNK.The IC 50 s of QL-X-138 against BTK, MNK1 and MNK2 kinases are 9.4 nM, 107.4 nM and 26 nM, respectively.The IC 50 s of QL-X-138 against Dengue 2 is 3.5 μM.QL-X-138 is used in the study of B-cell malignancies. QL-X-138 inhibits dengue virus 2 with an IC 50 of 3.5 μM. QL-X-138 can be used in the study of B-cell malignant tumors.

AMG PERK 44 is an orally active and selective PERK inhibitor (IC50: 6 nM) that induces autophagy.AMG PERK 44 inhibits GCN2 (IC50: 7300 nM) and B-Raf (IC50 >1000 nM) and can be used in the study of cancer.

CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.265 uM) respectively.

EG01377 2HCl is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1) with a Kd value of 1.32 μM and an IC50 value of 609 nM for both EG01377 2HCl against NRP1-a1 and NRP1-b1.EG01377 exhibits anti-angiogenic, antimigratory and antitumor activities.

Centrinone-B (LCR-323) is a potent and highly selective inhibitor of PLK4 (Ki: 0.59 nM).

Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

Doramapimod (BIRB 796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.

Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.

AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).

Tozasertib (MK-0457) is a pan-Aurora kinase inhibitor (Kis: 0.6/18/4.6 nM for Aurora A/Aurora B/Aurora C). It shows selectivity against more than 190 different kinases.

Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w (EC50s: 78.7/30.3/197.8 nM).

Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC50: 9 nM). X-376 also inhibits SY5Y neuroblastoma cells harboring ALK F1174L, MKN-45 gastric carcinoma cells harboring MET dependent, HepG2 cells and PC-9 lung cancer cell lines harboring EGFR exon 19 del with IC50s of 68 nM, 156 nM, 9.644 μM and 2.989 μM, respectively[1]. The effects of Ensartinib (X-396) in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that Ensartinib shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with Ensartinib at 25mg/kg bid. Ensartinib significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, Ensartinib appears well-tolerated in vivo. Mouse weight is unaffected by Ensartinib treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of Ensartinib, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of Ensartinib at 20, 40, 80 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 80mg/kg for Ensartinib. At NST levels, Ensartinib achieves an AUC of 66 μM×hr and a Cmax of 7.19 μM[1]. [1]. Lovly CM, et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinaseinhibitors. Cancer Res. 2011 Jul 15;71(14):4920-31.

Reversine, a small synthetic purine analogue (2, 6-disubstituted purine), is a potent inhibitior of Aurora A/B/C(IC50s=150-500 nM).

RAF709 is a novel Raf kinase inhibitor with IC50s of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.