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SOS1::KRAS
BI-3406

With KRAS::SOS protein-protein interaction inhibitor (PPIi) BI-3406 we share an unprecedented, highly potent and selective molecule for collaboration. Interested scientists from around the world are now invited to submit testable research proposals with our PPI inhibitor around novel disease indications until December 13, 2019.

β2AR
BI-167107

β2 adrenergic receptor (β2AR ) agonists have been used as bronchodilating agents for the last decades for the treatment of pulmonary diseases like asthma. BI-167107 was synthesized during a campaign to develop third generation of β2-agonists suitable for a once a day regimen. Due to its high potency and slow dissociation from the target it was subsequently used to support crystallization of active state β2AR and β2AR-G-protein complexes.

SYK
BI 1002494

Due to its high potency and good physicochemical properties, suitable selectivity profile and low toxicity, BI 1002494 is an excellent tool to explore SYK functions in vitro and in vivo.

STEP
BI-0314

With BI-0314 the first allosteric activator of tyrosine phosphatases is described. We hope to spark the design of selective allosteric ligands of phosphatases with the disclosure of the X-ray structure, and the elucidation of the mode of action of BI-0314 on STEP.

SMARCA2/4
ACBI1

ACBI1 causes degradation of the BAF chromatin remodeling complex proteins SMARCA2 and SMARCA4, as well to a lesser degree PBRM1.The compound is a PROTAC (proteolysis-targeting chimera) that induces degradation of its targets via inducing the formation of a triple complex of the target, the PROTAC, and the E3 ligase VHL, resulting in target ubiquitylation and proteasomal degradation.

sEH
BI-1935

BI-1935 is a potent and selective small molecule inhibitor of Soluble epoxide hydrolase (sEH). In a biochemical binding assay h-sEH it shows an IC50 of 7 nM and is also highly active in a cellular Hep G2-DHET assay format (IC50 < 1 nM).

PTK2
BI-3663

BI-3663 is a first in class low molecule weight degrader that tethers a highly selective PTK2 Kinase inhibitor BI-4464 to a CRL4CRBN E3 ubiquitin ligase ligand, aimed at triggering the intracellular destruction of the PTK2 protein. BI-3663 potently and rapidly induces reversible, long-lasting, and preferential removal of PTK2 in cells.

PTK2
BI-0319

We believe that BI-0319 is a valuable tool to effectively reduce PTK2 protein levels in cell lines to reveal and differentiate between kinase- dependent and -independent functions of PTK2.

PLK1
BI-2536

BI-2536 was the first potent and selective PLK1 inhibitor which entered clinical trials. It is a suitable in vitro and in vivo tool to study PLK function.

NSD3
BI-9321

BI-9321 is a potent and highly selective antagonist of the PWWP1 domain of NSD3. It is a first in class chemical probe, targeting the methyl-lysine binding site, developed in collaboration with the Structural Genomics Consortium (SGC). BI-9321 exhibits an in vitro potency of 200 nM and cellular target engagement at around 1 µM. In MOLM-13 cells BI-9321 downregulates Myc mRNA and impairs proliferation.

NMDA
BIII 277CL

BIII 277CL is a selective high affinity blocker of the NMDA receptor ion channel (Ki = 4.5 nM), which displayed beneficial effects in reducing the cortical infarct area in mice with focal cerebral ischemia.
We offer BIII 277CL to test biological hypotheses in vitro and in vivo.

NHE1
BI-9627

BI-9627 is a highly potent NHE1 inhibitor with low DDI potential, excellent pharmacokinetics, and good selectivity against NHE2 and NHE3.

Nav1.2
BIII 890CL

BIII 890CL is a highly potent, selective and use-dependent voltage-dependent sodium channel blocker suitable for in vitro and in vivo biological experiments. The compound has a high selectivity for site 2 of the sodium channel and preferentially binds to the inactivated state of the channel with an IC50 of 77 nM based on patch clamp evaluations. In contrast, the binding at the resting state is only 18 µM.

MMP-13
BI-4394

BI-4394 is a potent and highly selective inhibitor of MMP-13 that can be used as tool compound to test biological hypotheses in vitro.

According to the UK Third Generation Cannabinoid Act, the molecule cannot be shipped to the United Kingdom.

LFA-1
BI-1950

BI-1950 potently inhibits the binding of LFA-1 to ICAM-1 with a KD value of 9 nM and the production of IL-2 in human PBMC and whole blood with an IC50 value of 3 nM and 120 nM, respectively.

KRAS
BI-2852

The in vitro tool compound BI-2852 is a potent nanomolar inhibitor of the KRAS switch I/II pocket and directly inhibits both the active and inactive forms of KRAS.

HIV NNRT
BI-2540

BI-2540 is a potent inhibitor of HIV non-nucleoside reverse transcriptase (NNRT) and cross-reactive against clinically relevant mutants of reverse transcriptase. BI-2540 shows low clearance and good bioavailability upon p.o. dosing in rats. With BI-2439, a relatively close analog of BI-2540 with significantly lower activity (420-fold) is available as negative control for in vitro experiments.

HIV integrase
BI 224436

BI 224436 is the first non-catalytic-site integrase inhibitor (NCINI) reaching a clinical trial. It combines high solubility at all relevant physiological pH values with good cell permeability and good metabolic stability.

HCV NS3
BI-1388

BI-1388 is a nanomolar to picomolar inhibitor of HCV NS3 protease activity and of viral replication for various HCV genotypes and for resistant mutants D168V and R155K.

HCV NS3
BI-1230

BI-1230 is a single digit nanomolar inhibitor of HCV NS3 protease activity and of viral replication. BI-1230 was shown to be highly selective against other serine/cysteine proteases and to be suitable for in vivo studies.

HCV NS5B
BI 207127

BI 207127 (deleobuvir) is a highly potent inhibitor of the enzymatic function of NS5B, the RNA polymerase of HCV, and of viral replication  (~20 nM).

GSK-3
BI-5521

Our GSK-3 inhibitor BI-5521 with shown in vivo efficacy is characterized by high potency and good selecticvity.

GR
BI 653048

BI 653048 is a “dissociated” GR agonist (displaying different transcriptional regulatory profiles between gene transrepression and transactivation) with selectivity for other nuclear receptors (MR, PR) and good drug-like properties.

FLAP
BI 665915

BI 665915 demonstrates nanomolar FLAP binding potency and is a molecule suitable for testing biological hypotheses in vitro and also in vivo.

FAS
BI 99179

Our FAS in vivo tool compound BI 99179 is characterised by high potency, good selectivity and significant peripheral and central exposure upon oral administration in rats.

DPAP1
BI-2051

BI-2051 is a very potent inhibitor of the P. falciparum protease DPAP1. It inhibits recombinant DPAP1 with an IC50 of 0.3 nM and is highly selective versus the homologous human proteases CatC, CatK and CatL (all IC50 > 2500 nM). BI-2051 is highly soluble at pH 2.2, 4.5, 7 has a good cellular permeability and displays good in vitro PK properties in rats.

Chymase
BI-1942

Chymase plays an important and diverse role in the homeostasis for a number of cardiovascular processes and has been linked to heart failure. BI-1942 is a potent inhibitor of human chymase with an IC50 value of 0.4 nM and >100 fold selectivity against Cathepsin G and is thus a suitable tool for testing biological hypotheses involving human Chymase in vitro.

CDK8
BI-1347

Cyclin-dependent kinase 8 (CDK8) is a Mediator complex-associated transcriptional regulator.

CCR10
BI-6901

Our compound is the first small molecule inhibitor of the Chemokine receptor CCR10.1-3 It is a potent and selective compound and suitable for in vivo validation.

CCR1
BI 639667

BI 639667 is a potent, selective human CCR1 antagonist with optimized drug-like properties.

CTSC
BI-9740

BI-9740 is very potent, highly selective and orally bioavailable CatC inhibitor. BI-9740 shows no species selectivity and displays low nM IC50 in human, mouse and rat CatC assays. BI-9740 has high solubility at pH 2.2, 4.5 and 7. BI-9740 has very good in vitro and in vivo PK properties in several animal species (mouse, rat, mini pig).

Cathepsin C
BI-1750

BI-1750 is a stable and highly selective intracellular substrate for the human protease Cathepsin C (CatC).1 It can be used to monitor intracellular CatC activity in ex vivo whole blood assays or other cellular systems. This substrate works in whole blood assays from rats and minipigs as well.

BRD9
BI-9564

BI-9564 binds with high affinity to BRD9 KD(BRD9, ITC) = 14 nM and with lower affinity to closely related BRD7 KD(BRD7, ITC) = 239 nM. CECR2 was the only other identified off-target (KD(CECR2, ITC) = 258 nM), but with no effect in cells at 1 µM (FRAP assay). BI-9564 is completely negative on BET family members in the AlphaScreen (>100 µM).

BRD7/BRD9
BI-7273

BI-7273 is a potent dual BRD7/BRD9 inhibitor with 30 fold better potency in the BRD7 AlphaScreen assay compared to our more selective BRD9 inhibitor BI-9564.

BET PROTAC
MZ1

MZ1 is a first in class PROTAC (proteolysis-targeting chimeras) that tethers JQ1 to a VHL E3 ubiquitin ligase ligand, aimed at triggering the intracellular destruction of BET proteins. MZ1 potently and rapidly induces reversible, long-lasting, and preferential removal of BRD4 over BRD2 and BRD3 in cells.

BCL6
BI-3812

BI-3812 is a single digit nanomolar BCL6::Co-repressor inhibitor which also inhibits the BCL6::Co-repressor complex formation in cells (IC50 = 40 nM). BI-3812 is a classical PPI inhibitor probe compound for testing hypotheses around BCL6 biology in vitro.

BCL6
BI-3802

BI-3802 is a single digit nanomolar BCL6::Co-repressor inhibitor which induces efficacious BCL6 protein degradation in several Diffuse large B-cell lymphoma (DLBCL) cell lines (e.g., DC50 = 20 nM in SU-DHL-4 cells).

ATX
BI-2545

BI-2545 inhibits human ATX with an 50 of 2.2 nM. In human whole blood BI-2545 inhibits Autotaxin with an 50 of 29 nM and in rat whole blood with an 50 of 96 nM.

Aurora B
BI 831266

BI 831266 is a potent and selective Aurora B inhibitor that inhibits cell proliferation and could be used as tool compound testing biological hypotheses.

Alk5
BI-4659

BI-4659 is a potent and selective inhibitor of Alk5 (IC50 = 19 nM) which effectively blocks cellular phosphorylation of Smad2/Smad3 in HaCaT cells (EC50 = 185 nM). We also offer BI-4101 as negative control. BI-4659 (5 mg) can be ordered free of charge together with BI-4101.1,6