Ser/Thr Kinase Inhibitor

Ser/Thr Kinase Inhibitors (27):

Cat. No.	Product Name	Effect	Purity

HY-161111

KVS0001	Inhibitor	99.14%
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.

HY-132868

SLK/STK10-IN-1	Inhibitor	99.78%
SLK/STK10-IN-1 is a potent and selective inhibitor of SLK and STK10 with antitumor activity.

HY-103020

BAY-1816032	Inhibitor	99.73%
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.

HY-162426

UNC-CA2-103	Inhibitor	99.26%
UNC-CA2-103 (compound 128) is a potent inhibitor of Tousled like kinase 2 (TLK2), with the IC₅₀ of 18 nM.

HY-178207

DF-003	Inhibitor
DF-003 is a selective, orally active, ATP-competitive, and brain-penetrant ALPK1 inhibitor. DF-003 potently inhibits human ALPK1 and ALPK1[T237M] with IC₅₀s value of 1.5 nM and 16 nM. DF-003 exhibits more than 860-fold selectivity over the closest kinase. DF-003 inhibits TNF, CXCL10, or CXCL8 upregulation in HEK-293 cells. DF-003 can be used for the study of retinal dystrophy, optic nerve edema, splenomegaly, anhidrosis, and headache (ROSAH) syndrome.

HY-147655

CQ211	Inhibitor	99.58%
CQ211 is a potent and selective RIOK2 inhibitor with a K_d of 6.1 nM. CQ211 exhibits potent proliferation inhibition activity against multiple cancer cell lines.

HY-115677

ILK-IN-3	Inhibitor	99.62%
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.

HY-112158

NSC139021	Inhibitor	99.86%
NSC139021 (ERGi-USU) is a RIOK2 inhibitor with anticancer activity. RIOK2 can highly selectively inhibit the growth of ERG-positive cancer cells with IC₅₀s of 30-400 nM against cell lines. RIOK2 also causes cell cycle arrest and apoptosis in glioblastoma via induction of Skp2 and Skp2-p27/p21-Cyclin E/CDK2-pRb signaling.

HY-104001

BAY-524	Inhibitor	98.36%
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.

HY-115719

NR162	Inhibitor	99.7%
NR162 (compound 26) is a highly potent and selective CASK inhibitor (K_d of 22 nM).

HY-139893

ERGi-USU-6 mesylate	Inhibitor
ERGi-USU-6 mesylate (Compound 7b) is an inhibitor of ERG and RIOK2 (IC₅₀ values: 0.17 and 0.13 μM in VCaP cells, respectively). ERGi-USU-6 mesylate exhibits anticancer activity against ERG-positive prostate cancer.

HY-145725A

Baliforsen	Inhibitor
Baliforsen is an antisense oligonucleotide (16 nucleotides) designed to target myotonic dystrophy protein kinase (DMPK) mRNA and research myotonic dystrophy.

HY-116559

TIBI	Inhibitor	99.62%
TIBI is a potent and ATP-competitive inhibitor of Rio1 (IC₅₀: 0.09 μM, K_i: 0.05 μM). TIBI enhances the thermostability of the enzyme Rio1.

HY-12240

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

HY-W013852

PKC-IN-6	Inhibitor	99.63%
PKC-IN-6 (Compound 21) is a selective inhibitor of tyrosine and serine kinases. PKC-IN-6 shows inhibitory activity against PKC-α, PKC-δ, PKA, EGF-R with IC₅₀ values of 240, >500, >500, >100 μM, respectively. PKC-IN-6 is promising for research of cancers.

HY-173186

TLK1-IN-1	Inhibitor
TLK1-IN-1 (Compound 5n) is a TLK1 inhibitor with an IC₅₀ of 7.2 μM against TLK1B and a GI₅₀ of 2.7 μM in LNCaP cells. TLK1-IN-1 induces DNA damage and apoptosis in cancer cells, making it a potential candidate for prostate cancer research.

HY-172241

Tapencarium	Inhibitor
Tapencarium (RZL-012) is a serine/threonine kinase inhibitor. Tapencarium can reduce subcutaneous fat volume. Tapencarium is promising for research of fat-related disorders such as Dercum’s disease and aesthetic applications.

HY-175733

CQ3196	Inhibitor
CQ3196 is an orally active RIOK2 inhibitor with a K_d of 14 nM. CQ3196 effectively inhibits the ATPase activity of RIOK2, with an IC₅₀ value of 72 nM. CQ3196 inhibits cell proliferation and colony formation in gastric cancer cell lines. CQ3196 induces cell apoptosis in HGC-27 and AGS cells. CQ3196 suppresses downstream signal pathway of RIOK2. CQ3196 reduces phosphorylation of mTOR and AKT. CQ3196 modulates ribosome function and protein synthesis. CQ3196 inhibits tumor growth and can be used for gastric cancer invtro and invivo research.

HY-10424A

Milciclib maleate	Inhibitor
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.

HY-156792

RIOK2-IN-1	Inhibitor
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression.

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