Ser/Thr Kinase Inhibitor

TRULI (Lats-IN-1) is a potent and ATP-competitive inhibitor of Lats1 and Lats2 kinases. TRULI promotes Yap-dependent proliferation in postmitotic mammalian tissues.

KVS0001 is a selective SMG1 inhibitor. KVS0001 elevates the expression of transcripts and proteins resulting from truncating mutations. KVS0001 increased the presentation of immune-targetable HLA class I-associated peptides from nonsense-mediated decay (NMD)-downregulated proteins on the surface of cancer cells. KVS0001 exerts anti-tumor properties and can be studied in research for NMD-related diseases, including cancer and inherited diseases.

SLK/STK10-IN-1 is a potent and selective inhibitor of SLK and STK10 with antitumor activity.

BAY-1816032, a chemical probe, is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC₅₀ of 7 nM.

Epiblastin A is an ATP-competitive casein kinase 1 (CK1) inhibitor that inhibits CK1α, CK1δ, and CK1ε. Epiblastin A inhibits the kinase activity of STK10, BRSK1, EEF2K, EGFR, MKNK2, and RIPK2. Epiblastin A inhibits Ki-67 expression, induces Oct4-GFP expression, and enhances the conversion of mouse epiblast stem cells to embryonic stem cells. Epiblastin A selectively reduces the cell viability of colorectal cancer cell lines HCT116, HT29, and DLD1. Epiblastin A can be used in colorectal cancer-related research.

YM17 is an orally active TNIK inhibitor with an IC₅₀ of 181.9 nM and a K_d of 1.18 μM. YM17 induces Apoptosis and cell cycle redistribution. YM17 inhibits tumor growth in hepatocellular carcinoma xenograft models. YM17 can be used for research on hepatocellular carcinoma.

WNK2-IN-1 is a WNK2 inhibitor. WNK2-IN-1 inhibits the kinase activity of recombinant WNK2 in a dose-dependent manner, and simultaneously partially inhibits WNK3 and WNK4. WNK2-IN-1 modulates WNK2-SPAK downstream signaling by inhibiting WNK2-mediated SPAK phosphorylation, and further suppresses the proinflammatory transcriptional response induced by IL1β. WNK2-IN-1 can be used in studies related to the WNK2 signaling pathway and osteoarthritis.

VT02956 is a LATS inhibitor (IC₅₀: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids. VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC₅₀s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis.

ILK-IN-3 is an orally active integrin linked kinase (ILK) inhibitor. ILK-IN-3 improves the anticancer efficacy of Docetaxel (HY-B0011) in orthotopic LCC6 model.

NR162 is a selective CASK (Ca²⁺/calmodulin-dependent Ser/Thr kinase) inhibitor with an IC₅₀ of 80 nM and a Kd of 22 nM. NR162 shows about 50-fold selectivity for CASK than TYRO3. NR162 targets the unique GFG motif of CASK and has excellent shape complementarity to the CASK ATP binding pocket. NR162 can be used for the research of neurological diseases.

BAY-524 is a potent Bub1 kinase inhibitor. BAY-524 inhibits the recombinant catalytic domain of human Bub1 with an IC₅₀ of 450 nM. BAY-524 can be used for the research of anti-cancer in combination with other agents.

Baliforsen (ISIS 5987690) is an antisense oligonucleotide (ASO) that inhibits DMPK mRNA. Baliforsen binds within exon 9 of the human DMPK transcript to promote RNase H1-mediated degradation Baliforsen can be used for the research of myotonic dystrophy type 1.

B32B3 is an inhibitor of VprBP with an IC₅₀ value of 0.5 μM at the H2AT120p cell. B32B3 can suppress tumor growth.

Vibilsertib (Necrosis inhibitor 2) (Compound B19), a serine/threonine kinase inhibitor, is a cell necrosis inhibitor. Vibilsertib can be used to study diseases related to the necrosis pathway, including inflammation, tumors, metabolic diseases and neurodegenerative diseases.

SLK/STK10-IN-2 (Compound 23) is a highly selective STK10 inhibitor, with a K_d of 365 nM and an IC₅₀ of 0.85 μM. SLK/STK10-IN-2 exhibits EC₅₀ of 0.89 μM in NanoBRET cell experiments. SLK/STK10-IN-2 shows no significant binding to SLK, STK3/4. SLK/STK10-IN-2 can be used to study STK10-related diseases (such as abnormal lymphocyte migration).

Mtb against-2 is an (E)-4-oxocrotonic acid derivative that acts as an inhibitor of Mycobacterium tuberculosis protein kinase B (PknB). Mtb against-2 inhibits the growth of Mycobacterium tuberculosis in vitro, with an MIC of 0.82 μg/mL against Mycobacterium tuberculosis H37Rv. Mtb against-2 can be used in tuberculosis-related research.

SY-5102 is a potent, selective, and orally active cyclin-dependent kinase (CDK7) inhibitor with a K_d value of 0.03 nM. SY-5102 occupies the ATP-binding pocket of CDK7 via non-covalent binding to inhibit CDK7 activity, and downregulates its phosphorylation of cyclin CDK and RNA polymerase II. SY-5102 inhibits cancer cell proliferation, and induces tumor growth inhibition and regression. SY-5102 can be used in research related to triple-negative breast cancer.

Milciclib (PHA-848125) maleate is a cyclin-dependent kinase inhibitor that impairs melanoma cell growth and modulates gene expression involved in cell cycle regulation. Milciclib maleate has been shown to significantly affect the expression of various genes, including down-regulating PTTG1, contributing to its antiproliferative activity. Milciclib maleate enhances sensitivity to treatment in p53 mutated melanoma cells when combined with PTTG1 silencing.

Odemsertib etifosfate is a serine/threonine kinase inhibitor.