Kinases & Cell Signaling

Empesertib(BAY 1161909)

CAS 1443763-60-7

Empesertib(BAY 1161909) is a potent Mps1 inhibitor, with an IC50 of < 1 nM.

Vandetanib (ZD6474)

CAS 443913-73-3

Vandetanib is a potent inhibitor of VEGFR2 with an IC50 of 40 nM.

PF 6260933 dihydrochloride

CAS 1883548-86-4

PF 6260933 is a potent, selective and orally bioavailable MAP4K4 inhibitor with kinase IC50 of 3.7 nM, cell IC50 of 160 nM; possesses excellent kinome selectivity and suitable properties for in vivo pharmacological characterization; significantly improves…

Elenestinib

CAS 2505078-08-8

Elenestinib (BLU-263) is a potent and orally active tyrosine kinase inhibitor. Elenestinib has the potential for the research of systemic mastocytosis (SM).

AZD-1152-HPQA

CAS 722544-51-6

AZD1152-HQPA is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, and appr 3700 fold more selective for Aurora B over Aurora A.

Bezuclastinib

CAS 1616385-51-3

Bezuclastinib (PLX 9486; CGT9486) is a potent inhibitor of c-kit and c-kit D816V (0.0001<IC50<1 μM; extracted from patent WO2014100620 A2, compound P-2007). Bezuclastinib is a tyrosine kinase inhibitor.

LUNA18

CAS 2676177-63-0

LUNA18 is an 11-mer cyclic peptide inhibitor for the intracellular tough target RAS with Kd (KRAS/G12D) of 0.043 nM and cellular IC50 of 1.4 nM (AsPC-1). LUNA18 orally and dose-dependently exhibits potent anti-cancer activities in a mouse xenograft model.…

Axitinib

CAS 319460-85-0

Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.

ACBI3

CAS 2938169-76-5

ACBI3 is a selective, potent and in vivo active pan-KRAS PROTAC degrader, potently degrades 13 out of 17 of the most prevalent oncogenic KRAS alleles (DC50=3.9 nM in GP2d cells).

Rocaglamide (Rocaglamide A; Roc-A)

CAS 84573-16-0

Rocaglamide is a potent NF-κB activation inhibitor.

Saracatinib (AZD0530)

CAS 379231-04-6

Saracatinib (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk and shows high selectivity over other tyrosine kinases.

COTI-2

CAS 1039455-84-9

COTI-2 is a small molecule candidate anti-cancer drug which can convert mutant p53 to wild-type conformation.

Src kinase inhibitor I

CAS 179248-59-0

Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.

AZ-960

CAS 905586-69-8

AZ960 also inhibits many kinases less than 50% at a concentration of 0.1 μM such as JAK3 (IC50=9 nM), TrkA, Aurora, and ARK5. In cells, AZ 960 inhibits the phosphorylation of STAT5 in TEL-JAK2 cells with an average IC50 of 15 nM and exhibits 15-30 -fold…

NV-5138

CAS 2095886-80-7

NV-5138, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 possesses rapid antidepressant effects[1][2].

AC-003

CAS 2258671-03-1

AC-003 is a novel, orally administered small-molecule inhibitor targeting receptor-interacting protein kinase 1 (RIPK1), demonstrating therapeutic potential for the treatment of idiopathic pulmonary fibrosis (IPF).

HRX-0233

CAS 2409140-12-9

HRX-0233 (HRX0233) is a potent and selective inhibitor of MAP2K4 (MKK4), a kinase involved in the stress-activated protein kinase (SAPK) signaling pathway. MAP2K4 plays a role in regulating cellular responses to stress, apoptosis, and tumorigenesis. HRX-0233…

NSC319726

CAS 71555-25-4

NSC319726 is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.in vitro: For NSC319726, the effect was even greater as the IC50 for the 175 mutant was 8 nM…

VU0364739

CAS 1244639-78-8

VU0364739 is a selective inhibitor of phospholipase D2 (PLD2) with an IC50 value of 22 nM. Phospholipase D (PLD) enzymes, including PLD1 and PLD2, are involved in various cellular processes, such as signal transduction, membrane trafficking, and cytoskeletal…

JP-11646

CAS 1902983-63-4

JP-11646 is a novel potent, selective, non-ATP competitive Pim2 inhibitor with IC50 of 0.5/1/24 nM for Pim2/3/1, respectively; shows less potency for other kinases in a kinase selectivity panel; exhibits 4-760-fold greater suppression of MM proliferation and…

Sunvozertinib

CAS 2370013-12-8

Sunvozertinib is a potent inhibitor targeting the ErbB family of receptor tyrosine kinases, including EGFR (Epidermal Growth Factor Receptor) and Her2 (Human Epidermal Growth Factor Receptor 2), as well as BTK (Bruton's Tyrosine Kinase). It exhibits…

PF-07328948

CAS 2936625-34-0

PF-07328948 is a first-in-class branched-chain ketoacid dehydrogenase kinase (BDK) inhibitor with IC50 of 15 nM and shows a high degree selectivity over a number of kinases and other off-targets. PF-07328948 is the first known selective BDK inhibitor…

PT2385

CAS 1672665-49-4

PT-2385 is a selective HIF-2α antagonist with a Ki of less than 50 nM.

PZ09(PKC-9)

CAS 1132609-87-0

PZ09 (PKC-zeta inhibitor 9, PKC-ζ inhibitor PZ9) is a potent, isoform selective PKC-zeta (PKC-ζ) inhibitor with IC50 of 5.18 nM, displays excellent selectivity (>200-fold) over other PKC isoforms with exception of PKC-i (10-fold). PZ09 also shows high…

E722-2648

CAS 931963-55-2

E722-2648 (Compound C-1) is a novel specific and competitive small molecule β-catenin/BCL9 interaction inhibitor with ITC KD of 1.05 uM and IC50 of 9 uM, blocks oncogenic Wnt signaling and disrupts cholesterol homeostasis in colorectal cancer.E722-2648…

KY19382

CAS 2226664-93-1

KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used…

Gandotinib(LY2784544)

CAS 1229236-86-5

Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.

PF-07220060

CAS 2380321-51-5

PF-07220060 is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.

Divarasib

CAS 2417987-45-0

GDC-6036 is a novel oral KRAS G12C inhibitor.

AC3573

AC3573 (AC-3573) is a potent, specific small molecule inhibitor of HER3.AC3573 abrogates HER2–HER3 signalling in cells and is more specific for HER3, inhibits NRG (heregulin)-induced HER3 phosphorylation with IC50 of 10 uM, abrogates the formation of the…

SY-5609 (CDK7-IN-3)

CAS 2417302-07-7

SY-5609 (CDK7-IN-3) is a selective CDK7 inhibitor with a KD of 0.059 nM. CDK7-IN-3 shows poor inhibition on CDK2 (Ki=390 nM), CDK9 (Ki=290 nM), CDK12 (Ki=78 nM). CDK7-IN-3 induce apoptosis in tumor cells and has antitumor activity.

Molidustat(BAY 85-3934)

CAS 1154028-82-6

Molidustat (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3.

Exarafenib

CAS 2639957-39-2

Exarafenib (RAF/KIN_2787) is a potent, orally active pan-RAF inhibitor. Exarafenib has anticancer activity by suppression of downstream MAPK pathway signaling. Exarafenib can be used for cancer research.

NVS-ZP7-4

CAS 2349367-89-9

NVS-ZP7-4 is a potent ZIP7 Inhibitor, which inhibits Notch signaling with IC50 of 0.13 uM in HES-Luc reporter gene assays, selectively induces apoptosis and ER stress. NVS-ZP7-4 altered zinc in the ER, and an analog of the compound photoaffinity labeled ZIP7…

PREX-in1

CAS 674801-27-5

PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.

Allopole-A

CAS 3057557-03-3

Allopole-A is the first allosteric, specfic inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1) with IC50 of 2.5 nM in FP-based assays, Allopole-A is the active form of Allopole.

WAY-316606

CAS 915759-45-4

WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM.

UNC10225761A

CAS 945865-02-1

UNC10225761A is a multi-kinase inhibitor, cocktail of UNC10225387B, UNC10225263A and UNC10225761A, promotes stem-cell-like chimeric antigen receptor T cells (CAR T cells).

IWP-4

CAS 686772-17-8

IWP-4 is a small molecule Wnt inhibitor with an IC50 of 25 nM.

LMT-28

CAS 1239600-18-0

LMT-28 (LMT28) is a specific blocker of IL-6 signaling via inhibits IL-6Rβ (gp130) with IC50 of 5.9 uM (IL-6–induced luciferase activity), selectively inhibits IL-6–induced phosphorylation of STAT3, JAK2, and gp130; does not affect LIF-induced STAT3…

DC-TEAD3in03

DC-TEAD3in03 is a potent, selective, covalent TEAD3 inhibitor with IC50 of 0.16 uM, 100-fold selectivity over other TEAD isoforms (IC50>20 uM) in ABPP assays.DC-TEAD3in03 could significantly improve the thermal stability of TEAD3 protein, while it had minimal…

Napabucasin (BBI608)

CAS 83280-65-3

Napabucasin is a STAT3 inhibitor which blocks stem cell activity in cancer cells.

SP600125

CAS 129-56-6

SP600125 is a reversible and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively.

Aurora A Inhibitor I

CAS 1158838-45-9

Aurora A inhibitor I is a potent and highly selective Aurora A inhibitor with with an IC50 of 3.4 nM.

R406

CAS 841290-81-1

R406 is a competitive Syk inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value.

SAR-20347

CAS 1450881-55-6

SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.

Tofacitinib (CP-690550) Citrate

CAS 540737-29-9

Tofacitinib citrate is a JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively.

NSC59984

CAS 803647-40-7

NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway. The EC50 of NSC59984 in most cancer cells is significantly lower than those of normal cells, with EC50 of 8.38 μM for p53-null HCT116 cells.