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.

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.

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).

SY-5102 is a potent, selective and orally active cyclin-dependent kinase (CDK7) inhibitor with a K_d of 0.03 nM. SY-5102 shows anti-proliferative activity against HCC70 cells with an EC₅₀ of 9 nM. SY-5102 can inhibit CDK7-mediated CAK function (downregulate CDK2 Thr160 phosphorylation) and TFIIH transcription function (downregulate RNA polymerase II Ser5 phosphorylation). SY-5102 can induce G2/M cell cycle arrest, downregulate the expression of the oncogene c-Myc, and ultimately trigger cancer cell apoptosis. SY-5102 can be used for the research of triple-negative breast cancer (TNBC).

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.

ILK-IN-4 (compound 49) is an integrin-linked kinase (ILK) inhibitor. ILK-IN-4 can be used for cancer research.

UNC10112785 is a serine/threonine kinase inhibitor with a human GSK-3β IC₅₀ of 0.031 μM, human CDK-2 IC₅₀ of 0.016 μM, and human CDK-4 IC₅₀ of 1.99 μM. UNC10112785 can be used for the research of type 2 diabetes.

Protein kinase inhibitor 16 exhibits inhibitory activity against a variety of Ser/Thr kinase or receptor or non-receptor tyrosine kinase.

IMB-YH-8 is a serine/threonine protein kinase (PknB) inhibitor. IMB-YH-8 has strong antibacterial activity against Mycobacterium tuberculosis (MIC = 0.25 µg/mL). IMB-YH-8 can be used in the research of tuberculosis.

Anti-neuroinflammation agent 3 (Compound A.10.3) exhibits inhibitory activity against a variety of Ser/Thr kinase or receptor or non-receptor tyrosine kinase.

STK16-IN-1 (Standard) is the analytical standard of STK16-IN-1 (HY-101270). This product is intended for research and analytical applications. STK16-IN-1 is a STK16 kinase inhibitor with an IC50 of 295 nM.