Kinases & Cell Signaling

QNZ(EVP4593)

CAS 545380-34-5

QNZ shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. EVP4593 is a neuroprotective inhibitor of SOC channel.

MRTX849(Adagrasib)

CAS 2326521-71-3

MRTX849 is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound…

AT7867

CAS 857531-00-1

AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.

Flavopiridol Hydrochloride

CAS 131740-09-5

Flavopiridol Hydrochloride is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.

Y15

CAS 4506-66-5

Y15 is a direct and specific inhibitor of FAK auto-phosphorylation.

CT7001(Samuraciclib hydrochloride）

CAS 1805789-54-1

CT7001 hydrochloride is a selective CDK7 inhibitor, with IC50s of 41 nM and 578 nM for CDK7/CycH/MAT1 and CDK2/cycE1, respectively.

GSK840

CAS 2361146-30-5

Novel potent and selective RIP3 kinase inhibitor

Pazopanib Hydrochloride

CAS 635702-64-6

Pazopanib Hydrochloride is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

BMS-5

CAS 1338247-35-0

BMS-5 is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.

M2698

CAS 1379545-95-5

M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity[1].

PF-04217903

CAS 956905-27-4

PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant).

SQ22536

CAS 17318-31-9

SQ22536 is an effective adenylate cyclase (AC) inhibitor.

Cyclo(-RGDfK)

CAS 161552-03-0

Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Sequence: Cyclo(Arg-Gly-Asp-Phe-Lys).

ANA-12

CAS 219766-25-3

ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively.

MKK7-COV-3

MKK7-COV-3 (MKK7 Covalen inhibitor 3) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 5 nM, displays >1,000-fold selectivity over MKK4 (IC50=7.81 uM), shows EC50 of 1.3 uM for reduction of p-JNK in ICW assays in Beas2B cell line, without…

Doramapimod (BIRB-796)

CAS 285983-48-4

Doramapimod (BIRB 796) is a highly potent p38 MAPK inhibitor with an IC50 of 4 nM. It also inhibits B-Raf with an IC50 of 83 nM.

SB-590885

CAS 405554-55-4

SB-590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases.

WZ8040

CAS 1214265-57-2

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR…

ML-348(ML348)

CAS 899713-86-1

ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM), Exhibits 14-fold selectivity for LYPLA1 over LYPLA2, Also selective over a panel of ~30 other serine hydrolases.target: LYPLA1 [1]IC 50： 210 nM [1]

SC-79

CAS 305834-79-1

SC79 is a selective and cell-permeable Akt activator which activates Akt phosphorylation and inhibits Akt membrane translocation.

CP-673451

CAS 343787-29-1

CP-673451 is a potent and selective inhibitor of PDGFR with IC50s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.

LY2603618(IC-83)

CAS 911222-45-2

LY2603618 is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.

Tivozanib(AV-951)

CAS 475108-18-0

Tivozanib (AV-951; KRN951) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 0.21, 0.16, and 0.24 nM in cell assay, respectively.

Prexasertib (LY2606368) 2HCl

CAS 1234015-54-3

Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase, with IC50s of <1 nM and 8 nM for CHK1 and CHK2, respectively, and a Ki of 0.9 nM against purified CHK1.

G-749

CAS 1457983-28-6

G-749 is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants with IC50s of 0.4/0.6/3.5/7.5 nM for Wt Flt3/D835Y/MV4-11/Molm-14 respectively.G-749 showed potent and sustained inhibition of the FLT3 wild type and…

Pemigatinib

CAS 1513857-77-6

Pemigatinib is a selective FGFR inhibitor in development for the treatment of patients with cholangiocarcinoma.

PLX5622

CAS 1303420-67-8

PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals[1].

Selpercatinib(LOXO-292)

CAS 2152628-33-4

Selpercatinib is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 163, has an IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), respectively[1]. Antineoplastic activity[2].

EMD638683

CAS 1181770-72-8

EMD638683 is a potent SGK1 inhibitor with an IC50 of 3 uM. The serum- and glucocorticoid-inducible kinase 1 (SGK1) is transcriptionally upregulated by mineralocorticoids and activated by insulin. EMD638683 could serve as a template for drugs counteracting…

Alflutinib (AST2818 mesylate)

CAS 2130958-55-1

AST2818 mesylate is an EGFR inhibitor.

1-NM-PP1

CAS 221244-14-0

1-NM-PP1 is a cell permeable protein kinase D (PKD) inhibitor with an IC50 of 0.398 μM.

PF-562271 besylate

CAS 939791-38-5

PF-562271 (besylate) is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase with IC50 of 1.5 nM and 13 nM, and has > 100-fold selectivity against other protein kinases, except for some CDKs.

KX2-391

CAS 897016-82-9

KX2-391 is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

Casein Kinase inhibitor A51

CAS 2079068-74-7

Casein Kinase inhibitor A51 (CKIα inhibitor A51) is a novel pan-specific CKI (CSNK1) inhibitor (Kd=0.5-20 nM, CKIα Kd=5.3 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19; target…

Mobocertinib(TAK-788)

CAS 1847461-43-1

Mobocertinib is a potent epidermal growth factor receptor (EGFR) inhibitor and an antineoplastic agent, extracted from patent WO2019222093A1, compound A[1][2].

LY3023414

CAS 1386874-06-1

LY3023414 potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. LY3023414 potently inhibits mTORC1/2 at…

Enzastaurin (LY317615)

CAS 170364-57-5

Enzastaurin is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.

Taselisib（GDC-0032）

CAS 1282512-48-4

GDC-0032 is a potent, next-generation β iso Form-sparing PI3K inhibitor targeting PI3Kα/δ/γ with IC50 of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ. IC50 Value: 0.29 nM/0.12 nM /0.97 nM(PI3Kα/δ/γ) Target: PI3K in vitro: GDC-0032 is an orally…

Asp-3026

CAS 1097917-15-1

ASP3026 is a novel and selective inhibitor for ALK (anaplastic lymphoma kinase) with IC50 of 3.5 nM.

BAY 61-3606 (dihydrochloride)

CAS 648903-57-5

BAY 61-3606 (dihydrochloride) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase (IC50=10 nM) with no inhibitory effect on Btk, Fyn, Itk, Lyn, and Src.

PF4618433

CAS 1166393-85-6

PF-4618433 is a potent and selective PYK2 inhibitor, with an IC50 of 637 nM. PF-4618433 may be suitable for the research of osteoporosis, craniofacial and appendicular skeletal defects and for targeted bone regeneration[1][2].

GGTI 2418

CAS 501010-06-6

GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces…

CH5183284 (Debio-1347)

CAS 1265229-25-1

CH5183284 is an orally available and selective FGFR inhibitor with IC50s of 9.3, 7.6, and 22 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

AKI603

CAS 1432515-73-5

A novel small molecule Aurora A kinase inhibitor with IC50 of 12.3 nM, also inhibits Aurora B kinase activity to a less extent; disrupts normal spindle structure, and induces cell-cycle arrest; suppresses stem cell properties in breast cancer cells, and also…

ONO-4059(Tirabrutinib)

CAS 1351636-18-4

Tirabrutinib (ONO-4059) is a highly selective, orally bioavailable BTK inhibitor with an IC50 of 2.2 nM.

Belvarafenib

CAS 1446113-23-0

Belvarafenib is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.

TNO155

CAS 1801765-04-7

TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors[1].

GSK481

CAS 1622849-58-4

GSK481 can inhibit RIP1 WT S166 phosphorylation in human vs mouse plasmids overexpressed in HEK293T cellsGSK'481 have approximately equivalent RIP1 FP potencies against human andcynomolgus monkey RIP1 but was >100-fold less potent against nonprimate RIP1