type i kinase

PF-6689840 is a potent and selective Type II PTK6 Brk inhibitor with IC50 of 54 nM in biochemical assays; inhibits PTK6 phosphorylation at Y342 in engineered HET293T cells overexpressing PTK6 WT with IC50 of 0.25 uM; demonstrates superior kinase selectivity compared to the Type I inhibitors; inhibits tumor cell growth, which is independent of PTK6 expression levels in cells.

HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1 2 and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells [1] [2] [3].

8-MA-cAMP (8-Methylamino-cAMP) is a cyclic adenosine monophosphate analog that acts as a site-selective PKA agonist, exhibiting similar affinity for the B site of both Type I and Type II protein kinase A. When used in conjunction with analogs that preferentially target site A, such as 8-piperidinyl cAMP, 8-MA-cAMP facilitates selective stimulation of Type I enzymes.

A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC 50 s of 12 nM, 45 nM and 7.5 nM against the ALK5, ALK4 and ALK7 induced transcription, respectively [1].

Rp-8-CPT-cAMP is a structural combination of the lipophilic and non-hydrolyzable cAMP analogs, 8-CPT-cyclic AMP and Rp-cyclic AMPS .[1] It functions as a site-selective inhibitor of protein kinase A (PKA) type I and II, with preference towards site A of type I and site B of type II.2 By occupying cAMP binding sites at the regulatory subunit of PKA, Rp-8-CPT-cAMP prevents the kinase holoenzyme from dissociative activation.[2],[3]

8-Br-PET-cGMP is an agonist of type I cyclic GMP-dependent protein kinase (cGKI), which promotes the dimerization and activation of the catalytic activity of cGKI by binding to its regulatory domain. This compound is utilized to investigate the role of the cGMP signaling pathway in cell growth, vasodilation, and smooth muscle cell functions.

LY2857785 is a type I competitive and reversible ATP kinase inhibitor against CDK7 CDK8 CDK9 (IC50s: 246 nM 16 nM 11 nM).

R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.

SCH772984 HCl is a selective inhibitor of ERK1 2 that displays behaviors of both type I and type II kinase inhibitors, with IC50s of 4 and 1 nM, respectively. SCH772984 HCl has nanomolar cellular potency in tumor cells with mutations in BRAF, NRAS, or KRA

KN-93 hydrochloride is a cell-permeable, reversible, and competitive inhibitor of calmodulin-dependent kinase type II (CaMKII) with a K_i of 370 nM.

A 77-01 is a potent inhibitor of the TGF-(beta) type I receptor superfamily activin-like kinase ALK5, with an IC50 of 25 nM.

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).

TGFβRI-IN-1 is an orally active and selective inhibitor of TGFβ receptor type I (TGFβRI) kinase, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively.

TGFβRI-IN-4 is a potent, orally active TGFβ receptor type I kinase (TGFβRI) inhibitor that targets ALK5 (IC50: 44 nM) and NIH3T3 (IC50: 42.5 nM), inhibiting tumor growth and weight in a xenograft tumor model.

LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively. LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors ALK2 and ALK3 in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively, and was 200-fold more selective for BMP than for TGF-β.

LY550410 is a small molecule that acts as an ATP-competitive type I TGF-β receptor kinase inhibitor (type ITGF-β receptorkinase) featuring a heteroaromatic ring, which can effectively bind to the active site of the kinase domain. This compound regulates the TGF-β signaling pathway, thereby influencing gene expression and ultimately promoting cell growth. LY550410 holds potential for use in cancer research.

2'-Deoxyguanosine 5'-monophosphate (dGMP) is used as a substrate of guanylate kinases to generate dGDP, which in turn is phosphorylated to dGTP, a nucleotide precursor used in DNA synthesis. In addition, dGMP can be efficiently phosphorylated by the type I thymidylate kinase of the malarial agent P. falciparum. In humans, deficiency of mitochondrial deoxyguanosine kinase, which synthesizes dGMP from ATP and deoxyguanosine, contributes to mitochondrial DNA depletion syndrome.

Tuspetinib (HM43239) hydrate is a selectively active FLT3 inhibitor for oral administration, demonstrating IC₅₀ values of 1.1 nM for FLT3 WT, 1.8 nM for FLT3 internal tandem duplication (ITD), and 1.0 nM for FLT3 D835Y kinases. As a reversible type I inhibitor, it suppresses FLT3 kinase activity and influences signaling pathways including p-STAT5, p-ERK, SYK, JAK1 2, and TAK1. Additionally, Tuspetinib hydrate inhibits leukemic cell proliferation and triggers apoptosis [1] [2] [3].

VI 16832 is a broad-spectrum Type I kinase inhibitor, used for comparative expression analysis of protein kinases in various cancer cell lines.