GNE-493
CAS 1033735-94-2
GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
Kinases & Cell Signaling
Kinase inhibitors and modulators of intracellular signaling pathways.
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Kinases & Cell SignalingKinase inhibitors and modulators of intracellular signaling pathways.936 products →Epigenetics & Gene RegulationChromatin, transcription and epigenetic regulation.277 products →DNA Damage, Repair & Cell CycleDNA replication, repair, mitosis and cell-cycle regulation.228 products →Cell Death & AutophagyApoptosis, ferroptosis, necroptosis and autophagy research.117 products →Protein Degradation & ProteostasisPROTACs, molecular glues, ubiquitin systems, chaperones and proteostasis.173 products →Immunology & InflammationInnate and adaptive immunity, inflammatory pathways and immune signaling.297 products →NeuroscienceNeurotransmission, neural targets and neurological research.363 products →GPCRs & Receptor BiologyG-protein-coupled, nuclear and other ligand-binding receptors and their modulators.428 products →Ion Channels & TransportersIon channels, membrane transporters and pumps.196 products →Metabolism & EndocrinologyMetabolic enzymes, lipid and glucose metabolism and hormone signaling.404 products →Cardiovascular & HematologyVascular biology, coagulation, cardiac function, blood-pressure and hematology research.141 products →Anti-infectivesAntibacterial, antiviral, antifungal and antiparasitic research tools.202 products →Cancer ResearchCompounds with documented oncology research applications.530 products →ADCs & BioconjugationADC payloads, linkers, drug-linker conjugates and conjugation reagents.38 products →Probes & Assay ReagentsFluorescent and imaging probes, enzyme substrates and assay reagents.82 products →Natural ProductsNaturally occurring compounds for biological and chemical research.73 products →Cell Biology & Intracellular TransportCytoskeletal dynamics, endocytosis, vesicle trafficking, organelle function and cell differentiation.61 products →
Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
Kinases & Cell Signaling products
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ROSCOVITINE(Seliciclib)
CAS 186692-46-6
Roscovitine is a potent and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.
ICG-001
CAS 780757-88-2
ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. It works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM.
PF07104091(Tagtociclib)
CAS 2460249-19-6
PF-07104091 is an orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2), with potential antineoplastic activity. Upon administration, CDK2 inhibitor PF-07104091 selectively targets, binds to and inhibits the activity of CDK2. This may lead to cell…
Ral inhibitor 1
CAS 2249469-44-9
Ral inhibitor 1 is a covalent inhibitor of RalB (Ras-like GTPase) activation, inhibits guanine exchange factor Rgl2-mediated nucleotide exchange of Ral GTPase, selectively inhibits Ral over Ras; Ral inhibitor 1 inhibits RalB/Rgl2 interaction through covalent…
HG-14-10-04
CAS 1356962-34-9
HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.IC50 value: 20 nMTarget: ALKMore information can be found in the following Patent, Example 10Preparation of substituted pyrimidinamines as ALK kinase inhibitorsBy Aquila, Brian; Kamhi,…
AZD6244 (Selumetinib,ARRY-142886)
CAS 606143-52-6
Selumetinib is a highly potent MEK inhibitor, with an IC50 of 14 nM against MEK1.
TP-0903
CAS 1341200-45-0
TP-0903 is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.
Gartisertib
CAS 1613191-99-3
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
Senexin B
CAS 1449228-40-3
Senexin B is a potent, highly water-soluble and bioavailable CDK8/19 inhibitor, with Kds of 140 nM for CDK8 and 80 nM for CDK19.
Y-27632
CAS 146986-50-7
Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively.
RTA-408(Omaveloxolone)
CAS 1474034-05-3
RTA-408 is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO).
BT173
CAS 2232180-74-2
BT173 is a small molecule allosteric inhibitor of HIPK2-Smad3 interaction, specifically inhibits the TGF-β1/Smad3 pathway.BT173 disrupts HIPK2-Smad3 protein-protein interaction (PPI) without significant inhibition of HIPK2 kinase activity or inhibition of p53…
MRTX1133(MRTX-1133)
CAS 2621928-55-8
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRASG12D of 0.2 pM. MRTX1133…
MSU38225
CAS 1629160-83-3
MSU 38225 (MSU-38225) is a novel small molecule that inhibit the Nrf2 pathway, potentially inhibiting Nrf2 transcriptional activity and cancer cell growth; MSU38225 downregulates Nrf2 transcriptional activity and decreases the expression of Nrf2 downstream…
ST034307
CAS 133406-29-8
ST034307 is a potent and selective adenylyl cyclase 1 (AC1) inhibitor, with IC50 of 2.3 μM.
Hydrazinocurcumin
CAS 131068-23-0
Hydrazinocurcumin is a synthetic curcumin derivative that inhibits the proliferation of bovine aortic endothelial cells (BAECs) with IC50 of 520 nM without cytotoxicity, inhibits STAT3 phosphorylation and downregulates an array of STAT3 downstream targets;…
2OH-BNPP1
CAS 833481-73-5
2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.
SB02024
CAS 2126737-28-6
SB02024 is a novel highly potent, selective, ATP competitive, orally active inhibitor of vacuolar protein sorting 34 (Vps34) with Kd of 1 nM, >1000 times selective towards other PI3K isoenzymes; SB02024 is also highly selective at 1 uM in the DiscoveRx…
Onvansertib (NMS-P937)
CAS 1034616-18-6
NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.
AMG-548
CAS 864249-60-5
AMG-548 is a potent, oral and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γand p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM)…
BAY1125976
CAS 1402608-02-9
BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.
DW0254
CAS 2031162-89-5
DW0254 (DW-0254,DW 0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.DW0254…
Pacritinib citrate
CAS 1228923-42-9
Pacritinib Citrate is the citrate salt form of pacritinib, an orally bioavailable inhibitor of Janus kinase 2 (JAK2).
UNC10225387B
CAS 2650093-47-1
UNC10225387B is a multi-kinase inhibitor, cocktail of UNC10225387B, UNC10225263A and UNC10225761A, promotes stem-cell-like chimeric antigen receptor T cells (CAR T cells).
LY333531 Hydrochloride(Ruboxistaurin HCl)
CAS 169939-93-9
Ruboxistaurin hydrochloride is a selective and ATP-competitive PKCβ inhibitor, with IC50s of 4.7 and 5.9 nM for PKCβI and PKCβII, shows less potent inhibition on PKCη (IC50, 52 nM), PKCα (IC50, 360 nM), PKCγ (IC50, 300 nM), PKCδ (IC50, 250 nM), and has no…
VX-11e(TCS ERK 11e)
CAS 896720-20-0
VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.
BI-2493
CAS 2937344-16-4
BI-2493 is a structural analogue of BI-2865 and a highly selective pan-KRAS inhibitor. BI-2493 can attenuate tumor growth. BI-2493 can be used for cancer iseases research.
BAY1217389
CAS 1554458-53-5
BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.
BI-2865
CAS 2937327-93-8
BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 blocked nucleotide exchange to prevent the activation of wild-type KRAS and a broad range of KRAS mutants, including G12A/C/D/F/V/S, G13C/D, V14I, L19F, Q22K, D33E, Q61H, K117N and A146V/T. Inhibition of…
GDC-0077
CAS 2060571-02-8
GDC-0077 is an orally available PI3K inhibitor with potential antineoplastic activity. GDC-0077 is extracted from patent WO 2017001645 A1, formula I.
Ingenol 3-angelate
CAS 75567-37-2
Ingenol 3-Angelate is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.
SBP-3264
CAS 2869148-13-8
SBP-3264 (SBP3264) is a sepecific inhibitor of Hippo signaling pathway kinases STK3 and STK4 with low nanomolar potency. SBP-3264 specifically inhibited the Hippo signaling pathway in cultured mammalian cells and possessed favorable pharmacokinetic and…
MRTX 0902
CAS 2654743-22-1
MRTX0902 is a potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10).
Asciminib
CAS 1492952-76-7
Asciminib (ABL001) is a potent and selective allosteric Bcr-Abl inhibitor; inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
Ver-246608
CAS 1684386-71-7
Novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupting Warburg metabolism and inducing context-dependent cytostasis in cancer cells
BGB 15025
CAS 2766481-17-6
BGB-15025 is a potent and selective HPK1 inhibitor. It is used in the treatment of various cancers.
Pirtobrutinib (LOXO-305)
CAS 2101700-15-4
LOXO-305 is an investigational, novel, selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. LOXO-305 was designed to reversibly bind BTK, preserve activity in the presence of the acquired resistance, and avoid off-target kinases that have…
Pexidartinib hydrochloride (PLX-3397)
CAS 2040295-03-0
Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, selective and ATP-competitive CSF1R (cFMS) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related…
IAG933
CAS 2714434-21-4
IAG933 (IAG-933) is a potent, selective and orally efficacious YAP1/WWTR1(TAZ)-panTEAD protein-protein interaction inhibitor (YAP/TAZ-TEADs PPI), inhibits TEAD-driven transcriptional activity and displays anti-cancer effects.
Dorsomorphin dihydrochloride
CAS 1219168-18-9
Dorsomorphin dihydrochloride (BML-275 dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109±16 nM.
VT104
CAS 2417718-25-1
VT104 (VT-104) is a specific small molecule inhibitor of YAP/TAZ-TEAD-dependent transcription with IC50 of 10.4 nM in YAP reporter assay, pan-TEAD palmitoylation inhibitor.VT104 inhibited palmitoylation of both endogenous TEAD1, TEAD3 proteins in cells.VT104…
CSLP37
CAS 2244984-64-1
CSLP37 (RIPK2 inhibitor CSLP37) is a novel potent, ATP pocket-binding RIPK2 inhibitor with IC50 of 16.3 nM in ADPGlo assay, demonstrates inhibition of both the RIPK2-XIAP interaction, and of cellular and in vivo NOD2 signaling; exhibits inhibition of TNF…
TED-347
CAS 2378626-29-8
TED-347 (TED347) is an irreversible inhibitor of TEAD4-Yap1 protein-protein interaction (EC50=5.9 uM in FP asssays) via covalent modification of conserved cysteine (Cys367, Ki=1.3 uM), inhibits its binding to Yap1, blocked its transcriptional activity;…
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11β-HSD (1)15-PGDH (2)5-HT Receptor (16)Acetyl-CoA Carboxylase (ACC) (3)Acetylcholinesterase (AChE) (2)Ack1 (TNK2) (1)Acyltransferase (1)ADC Cytotoxin (6)ADCs Linker/Click Chemistry (5)Adenosine Receptor (9)Adenylate Cyclase (2)Adrenergic Receptor (11)Akt (12)Alcoholism (2)Aldehyde Dehydrogenase (ALDH) (6)Allergy (5)Alzheimer Disease (13)Aminopeptidase (1)AMPK (8)Amyloids (4)Anaplastic Lymphoma Kinase (ALK) (9)Androgen Receptor (AR) (11)Anemia (4)Angiotensin Receptor (4)Antibody/Protein labeling dyes (1)Antifolate (2)Anxiety (1)Apoptosis Inducer (3)Arginase (1)Arp2/3 complex (1)Aryl hydrocarbon Receptor (AhR) (1)Asthma (5)Atherosclerosis (2)ATM/ATR (8)Aurora Kinase (10)Autophagy (6)Autophagy-related Protein (Atg) (2)Autotaxin (2)Bacterial (26)Bacterial Infection (17)Bcl-2 (14)Bcr-Abl (5)BCRP (1)Beta-catenin (4)Beta-secretase (BACE) (4)Blood Cancer (91)BMI-1 (1)Bone Cancer (6)Brain Cancer (6)Breast Cancer (30)Bromodomain (22)BTK (10)c-Fms (CSF1R) (5)c-Fos/AP-1 (1)c-Kit (6)c-Met (HGFR) 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