protein kinases

Necrostatin-1 (Nec-1) is a specific RIP1 inhibitor and necrotic apoptosis inhibitor, which inhibits TNF-α-induced necrotic apoptosis and also inhibits IDO.

CC214-1 is an mTOR inhibitor with potential anticancer activity, inhibits protein translation, and induces autophagy. CC214-1 is an in vitro tool compound for exploring the biology of mTOR kinases and can be used to study myeloma.

Lidocaine hydrochloride (Lignocaine hydrochloride) is a local anesthetic and cardiac depressant used as an antiarrhythmic agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK p38 MAPK signaling pathways in the murine macrophages.

Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.

Honokiol (NSC-293100) is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1 ERK2.

Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms (IC50=10 30 47 84 74 140 146 nM). Pazopanib has antitumor activity.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx.

Trifluoperazine dihydrochloride (SKF5019) is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic.

Urolithin B is one of the gut microbial metabolites of ellagitannins and is found in diverse plant foods, including pomegranates, berries, walnuts, tropical fruits, and medicinal herbs. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. Urolithin B has anti-inflammatory and antioxidant effects.

Palbociclib monohydrochloride (PD 0332991 hydrochloride) is a selective inhibitor of CDK4 6 (IC50s: 11 16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

Palbociclib Isethionate (PD 0332991 isethionate) is a selective inhibitor of CDK4 6 (IC50s: 11 16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property.

(-)-Bornyl acetate (L-(-)-Bornyl acetate) is a less active enantiomer of (+)-Bornyl acetate. Isolated from hyssop oil, it possesses antifungal, highly active whitening, and antioxidant properties, and it has potential applications in cosmeceutical materials. It downregulates proinflammatory cytokines in vitro and in vivo, reduces the number of total cells, neutrophils, and macrophages in BALF, attenuates histologic lung alterations, decreases the wet-to-dry weight ratio in BALF, and inhibits the activation of NF-kappa-B inhibitor alpha, extracellular regulated protein kinases, c-JunN-terminal kinase, and p38 mitogen-activated protein kinase.

(+)-Isocorydine hydrochloride (Isocorydine HCl) is a eukaryote protein kinases Inhibitor.

Imatinib impurities3 is a protein kinases inhibitor with IC50 values of 6.95uM, 0.245uM, 0.139uM for ABL1 wt, KIT wt, PDGFRR wt, respectively.

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

N-phenylthiophene-2-carboximidamide is a thiophene derivative that functions as an inhibitor of protein tyrosine kinases (PTKs) and a ligand for G protein-coupled receptors (GPCRs).

mTOR inhibitor 9d is a dual inhibitor of the protein kinases mTOR and PI3K with an mTOR IC50 value of 0.31 nm, and can be used for the treatment of leukemia, skin cancer, breast cancer, lung cancer and colon cancer.

AMARA peptide acetate is a substrate for SIK and AMPK.AMARA peptide is a minimal substrate of several members of the protein kinases family. It consists of the phosphorylation site for AMP-activated Protein Kinase (AMPK).

IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.

ARN25068 is a potent inhibitor of GSK-3β, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].

GSK2983559 free acid is an effective and selective inhibitor of receptor-interacting protein 2 (RIP2). GSK2983559 free acid shows excellent activity in blocking many proinflammatory cytokine responses in human inflammatory bowel disease explant samples an

JNK3 Inhibitor-4, a potent 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile derivative, demonstrates a strong inhibitory effect on JNK3 with an IC 50 value of 1.0 nM. It exhibits exceptional selectivity against JNK3 when compared to other protein kinases, including isoforms JNK1 (IC 50 = 143.9 nM) and JNK2 (IC 50 = 298.2 nM). Additionally, JNK3 Inhibitor-4 benefits from neuroprotective properties and is predicted to permeate the blood-brain barrier effectively.

Necroptosis-IN-1 is a potent necroptosis inhibitor of RIPK1. It is an analog of Necrostatin-1.

Olomoucine is an ATP-competitive inhibitor of Cdk2 cyclin A, Cdc2 CyclinB, CDK2 CyclinE, CDK5 p35, and ERK1 p44 MAP kinase with IC50s of 7, 7, 7, 3, and 25 µM, respectively. It regulates the cell cycle and exhibits anti-melanin tumor activities.

PD 198306 is a selective inhibitor of MAPK ERK-kinase (MEK) with antihyperalgesic effects. PD 198306 reduces the Streptozocin-induced increase in the level of active ERK1.

ROCK-IN-5 (compound I-B-37) is a potent inhibitor of protein kinases, including ROCK, ERK, GSK, and AGC, with potential applications in cardiac, proliferative, and neurodegenerative disease research.

GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor that binds to the RIP3 kinase domain (IC50: 0.9 nM) and inhibits kinase activity (IC50: 0.3 nM).

MS67 is a potent and selective degrader of WD40 repeat domain protein 5 (WDR5) with a dissociation constant (Kd) of 63 nM, exhibiting no activity against protein methyltransferases, kinases, G-protein-coupled receptors (GPCRs), ion channels, and transporters, and notably demonstrating significant anticancer properties.

GSK-872 (GSK2399872A) is an effective and specific RIP3 kinase inhibitor. It binds RIP3 kinase domain with high affinity (IC50: 1.8 nM) and inhibits kinase activity (IC50: 1.3 nM).

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1 26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.

CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].

GSK2983559 active metabolite (RIPK2-IN-1) is a potent, selective receptor-interacting protein-2 (RIP2) kinase inhibitor.

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor, with IC50 values of 0.5 nM for PI3Kα, 0.7 nM for PI3Kδ, 3.7 nM for PI3Kβ, and 6.4 nM for PI3Kγ. It exhibits superior antitumor activity and demonstrates more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.

Trifluoperazine (trifluoroperazine) is a Dopamine D2 receptor inhibitor(IC50 : 1.2 nM), and Treatment of schizophrenia.

KN-62 is a potent and specific Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μM.

RIPA-56 is an inhibitor of RIP1

LFM-A13（IC50=2.5 μM）, a specific Bruton's tyrosine kinase (BTK), is more than 100-fold specificity than other protein kinases, such as JAK1, JAK2, HCK, EGFR, and IRK.

STO-609 is a specific and cell-permeable inhibitor of the Ca2+ calmodulin-dependent protein kinase kinase (CaM-KK) for recombinant CaM-KKα KKβ (Ki: 80 15 ng mL).

PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.

A-484954 (A 484954) is a highly specific eukaryotic elongation factor-2 (eEF2, IC50: 280 nM) inhibitor.

Piceatannol (Astringenin) is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expression of TNF-induced. It is synthetic from the conversion of resveratrol by cytochrome P450 1B1.

ICCB-19 hydrochloride (ICCB-19 HCl) is an inhibitor of TRADD (TNFRSF1A Associated Via Death Domain). It binds to a pocket on the N-terminal TRAF2-binding domain of TRADD (TRADD-N), which interacts with the C-terminal domain (TRADD-C) and TRAF2 to modulate the ubiquitination of RIPK1 and beclin 1.

KN-93 is a selective inhibitor of Ca2+ calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase.

Necrostatin 2 racemate (Necrostatin-2 racemate) is an potent and specific inhibitor of RIPK1.

(±)-1,2-Diolein [1,2-Dioleoyl-rac-glycerol] is a PKC activator that can increase Ca²⁺ influx in myotubes.