TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.

Brivanib is an ATP-competitive inhibitor against human VEGFR2 and FGFR with IC50 of 25 nM and 148 nM, respectively.

Emupertinib (example 37) is a potent EGFR inhibitor with IC50 values of <0.3 nM, 0.52 nM, 0.5 nM, 0.69 nM and 0.92 nM for EGFR (d746-750/T790M/C779S), EGFR (L858R/T790M/C797S), EGFR (d746-750/C797S), EGFR (L858R/C797S), and EGFR (wild-type), respectively.

IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk with an IC50 of 0.5 nM.

PD168393 is potent, cell-permeable, irreversible and selective inhibitor of EGF receptor (EGFR) tyrosine kinase and ErbB2.

Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1-4 with IC50 values of 1.2, 2.5, 3.0 and 5.7nM, respectively.

Risvodetinib is a potent protein tyrosine kinase inhibitor. Risvodetinib involves in synthesis of Abelson protein kinases (c-Abl1, c-Abl2, and c-kit) inhibitor.

I3IN-002 is a small-molecule RNA-binding protein IGF2BP3 inhibitor with an IC50 value of approximately 2 μM in SEM cells. I3IN-002 interferes with interaction with m6 A-modified mRNAs, disrupting the stabilization of target genes (such as CDK6, MYC, and BCL2) to inhibit leukemic cell growth, induce cell cycle arrest, and promote apoptosis. I3IN-002 is promising for research of B-cell acute lymphoblastic leukemia.

Papaveroline is a Fyn Tyrosine Kinase inhibitor. Papaveroline can be used for the research of neurological disease, such as Alzheimer's disease (AD).

RD0392 (Compound 5) is a competitive tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC50=1.3 nM). RD0392 is promising for research of neurodegenerative diseases like Alzheimer’s.

Lysoganglioside-GM1 (LysoGM1) ammonium is a derivative of Monosialoganglioside GM1, which lacks a fatty acid. Lysoganglioside-GM1 ammonium is also an inhibitor of GM1 aggregation. Lysoganglioside-GM1 ammonium can inhibit the activation of Lyn and laminin-1-mediated neurite outgrowth. Lysoganglioside-GM1 ammonium can be used in the research of nervous system diseases.

BBT-176 is an orally effective EGFR inhibitor. BBT-176 has inhibitory activity against multiple EGFR C797S mutant cell lines. BBT-176 is commonly used in cancer research.

BIEGi-1 is an EGFR inhibitor. BIEGi-1 effectively disrupts the EGFR-Rheb interaction in cells. BIEGi-1 robustly inhibits EGFR kinase activity (reduces p-Y1068-EGFR) as well as mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant cells. BIEGi-1 shows strong antiproliferative effects on EGFR-mutant PC9 and HCC827 cells with IC50 values of 17 nM and 20 nM, respectively. BIEGi-1 can be used for the study of cancers harboring EGFR mutations, such as non-small cell lung cancer (NSCLC).

AP-24226 is a potent inhibitor of Scr/ABL.

LPS-123 is a covalently irreversible BTK inhibitor with an IC50 of < 5 nM. LPS-123 simultaneously inhibits the catalytic activity of BTK at Tyr551 and its self-activation at Tyr223. LPS-123 inhibits phosphorylation of the AKT/mTOR and MAPK signaling pathways, activation of PLCγ2, ERK1/2, p38, AKT, and mTOR, and blocks the production of CCL3 and CCL4 chemokines. LPS-123 exhibits significant anti-proliferative activity against various B-cell lymphoma cell lines and effectively induces apoptosis via a caspase-dependent pathway. LPS-123 also demonstrates significant antitumor activity in the OCI-Ly7 xenograft model. LPS-123 can be used for lymphoma research.

4-TCPA is a potent VEGFR2 inhibitor. 4-TCPA induces apoptosis and cell cycle arrest, likely through inhibition of VEGFR2 and EGFR signaling with additional effects on the mTOR pathway. 4-TCPA can inhibit the vitality and proliferation of various cancer cell lines. 4-TCPA can be used for the study of cancers such as lung cancer, breast cancer and leukemia.

CRBN ligand-185 is a CRBN ligand. CRBN ligand-185 can be used as a target protein ligand for the synthesis of PROTACs targeting CRBN (Ligands for Target Protein for PROTAC), such as NX-5948.

HI042 is a FMS-like Tyrosine Kinase 3 (FLT3) inhibitor. HI042 shows IC50 values of 0.62 μM for MOLM-13, 0.33 μM for MV4-11, and 0.89 μM for OCI-AML3 cells. HI042 selectively reduces the viability of FLT3-internal tandem duplication (FLT3/TD) mutations-positive cell lines, induces apoptosis, disrupts cell cycle progression, and diminishes the clonogenic potential. HI042 can be used for the research of acute myeloid leukemia (AML).

TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTKWT), >40,000 nM (BTKC481S), 7.9 nM (TEC) and 12.4 nM (TXK). TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis.

EGFR ligand-14-PEG3-Boc contains EGFR ligand and linker. EGFR ligand-14-PEG3-Boc can be used for the synthesis of SJF-1521.

IHMT-15130 is a highly potent irreversible BMX kinase inhibitor (IC50=1.47 nM). IHMT-15130 inhibits the secretion of inflammatory cytokines, blocks inflammatory signaling pathways, and alleviates Angiotensin II-induced myocardial hypertrophy in mice. IHMT-15130 is promising for research of myocardial hypertrophy.

Midobrutinib (Example 13) is a BTK inhibitor (IC50: 0.813 nM). Midobrutinib can be used for research of diseases involving BTK, particularly cancer.

VS1150 (Compound 11) is a BCR-ABL-targeting phosphorylation-inducing chimeric small molecule (PHICS). VS1150 significantly inhibits oncogenic kinase BCR-ABL signaling by inducing inhibitory phosphorylation at its Y253 (EC50: 69 nM), subsequently triggering cell apoptosis. VS1150 also inhibits other oncogenic ABL fusions and drug-resistant mutants like T315I. VS1150 can be used for chronic myeloid leukemia (CML) and other ABL fusion-driven cancers research.

KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies.

Taligantinib (Compound Example 70) is an orally active and selective dual inhibitor targeting vascular endothelial growth factor receptor 2 (VEGFR-2) and hepatocyte growth factor receptor (c-Met). Taligantinib suppresses tumor angiogenesis and cell proliferation. Taligantinib is promising for research of solid tumors such as non-small cell lung cancer and hepatocellular carcinoma.

Pro-Dasatinib (compound 2j), an amino acid analog of Dasatinib, is a potent Src/Abl kinase inhibitor. Pro-Dasatinib has antiproliferative activity against K652 leukemia cancer cells with an IC50 of 0.21 nM.

CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27  nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia.

cis-NVP-ADW742 (cis-ADW742) is a cis isomer of NVP-ADW742. NVP-ADW742 is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.

SKS-927 is a Src kinase inhibitor, with an IC50 value of 3.9 nM. SKS-927 inhibits the proliferation of Src-transformed rat fibroblasta, with an IC50 value of 73 nM. SKS-927 exhibits an IC50 value of 720 nM against EGFR. SKS-927 can be used for the study of cancer and osteoporosis.