Kinases & Cell Signaling

SU11274 (PKI-SU11274)

CAS 658084-23-2

SU11274 is a selective Met inhibitor with IC50 of 10 nM, but has no effects on PGDFRβ, EGFR or Tie2.

Elimusertib hydrochloride (BAY 1895344 hydrochloride)

BAY-1895344 is a potent, orally available and selective ATR inhibitor, with IC50 of 7 nM. Anti-tumor activity[1].

Apatinib (free base)

CAS 811803-05-1

Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the treatment of advanced or metastatic gastric…

Verteporfin (1:1 regioisomer mixture)

CAS 129497-78-5

Verteporfin is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions.

MRT68921

CAS 1190379-70-4

MRT68921 is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.

GSK-3008348 HCl

CAS 1629249-40-6

GSK3008348 is an Integrin alphaV inhibitor.

PLX5622 hemifumarate

PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622…

BMS-599626 (AC480)

CAS 714971-09-2

AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc

MRT67307 HCl

MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively.

Ulixertinib (BVD-523, VRT752271)

CAS 869886-67-9

Ulixertinib (VRT752271) is a reversible, ATP-competitive inhibitor of ERK1 and ERK2 kinases, with IC50 of <0.3 nM against ERK2.

Rigosertib sodium

CAS 1225497-78-8

Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM; shows 30-fold greater selectivity against PLK2 and no activity to PLK3.

Deucravacitinib (BMS-986165)

CAS 1609392-27-9

Tyk2-IN-4 is a selective, potent, allosteric inhibitor of tyrosine kinase 2 (Tyk2).

PCI-29732

CAS 330786-25-9

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.IC50 value: 8.2 nM [1]Target: Btk kinasePCI 29732(compound 1) has a 8.2 nM potency against Btk in a FRET based biochemical enzymology…

NSC781406

CAS 1676893-24-5

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.

Pyrotinib dimaleate

CAS 1397922-61-0

Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 s of 13 and 38 nM, respectively.

Cerdulatinib (PRT062070; PRT2070)

CAS 1198300-79-6

Cerdulatinib (PRT062070) is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.

LDN-192960 dihydrochloride

CAS 184582-62-5

LDN-192960 is a potent Haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase) inhibitor with an IC50 of 0.010 µM.

Trilaciclib dihydrochloride (G1T28)

CAS 1977495-97-8

Trilaciclib hydrochloride is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.

NSC 23766 trihydrochloride

CAS 1177865-17-6

NSC 23766 trihydrochloride is an inhibitor of Rac1 activation.

NVP-BQR695 (BQR-695)

CAS 1513879-21-4

BQR-695 is a PI4KIIIβ inhibitor with IC50s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.

SCR-1481B1 (BMS-817378, bis-Tris salt)

CAS 1174161-86-4

SCR-1481B1 (c-Met inhibitor 2) is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.

Imatinib (free base)

CAS 152459-95-5

Imatinib is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.

Akt-I-1,2 HCl

CAS 473382-50-2

The compound (Akt-I-1,2) inhibited both Akt1 and Akt2 with IC50 values of 2.7 and 21 μM respectively. It does not inhibit AKT3. The compound is a reversible inhibitor, and exhibits a linear mixed-type inhibition against ATP and peptide substrate. In addition…

PF-719

CAS 1404454-02-9

PF-719 (PF719) is a potent, selective Pyk2 inhibitor with IC50 of 17 nM, displays 25-fold selectvity over FAK (IC50=469 nM); does not have significant inhibitory effects on recombinant MLCK2, p38, Akt1, or ROCK1, and very little inhibtion at Src family…