Warm Substances in Protease Inhibitor Library



CAS No. 133407-82-6

MG-132 is definitely an inhibitor of proteasome with IC50 of 100 nM inside a cellular-cost-free assay, plus inhibits calpain with IC50 of 1.2 μM.


CAS No. 179324-69-7

Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of .6 nM within a cell-totally free assay.


CAS No. 868540-17-4

Carfilzomib (PR-171) is undoubtedly an irrevocable proteasome inhibitor with IC50 of 5 nM in ANBL-6 tissue, exhibited preferential in vitro inhibitory power versus the ChT-L exercise in the β5 subunit, but a minimum of impact on the PGPH and T-L pursuits.

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Very hot-offering Inhibitors

Rock and roll and roll inhibitor

Y-27632 dihydrochloride

Y-27632 dihydrochloride is truly a specific ROCK1 (p160ROCK) inhibitor with Ki of 140 nM, uncovers>200-fold selectivity over other kinases, that come with PKC, camp out out-centered healthful protein kinase, MLCK and PAK.

Relevant Products: Thiazovivin, Fasudil (HA-1077) HCl

GSK-3 inhibitor


CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, and that is certainly certainly a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM capacity to specific GSK-3 as well as its nearest homologs Cdc2 and ERK2.

Linked Products: SB216763 , CHIR-98014

Proteasome Inhibitor


MG-132 is unquestionably an inhibitor of proteasome with IC50 of 100 nM, and likewise inhibits calpain with IC50 of 1.2 μM.

Connected Goods: Carfilzomib (PR-171) , ONX-0914 (PR-957)

HDAC Inhibitor

Romidepsin  (FK228, Depsipeptide)

Romidepsin  (FK228, depsipeptide) could be a highly effective HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM, correspondingly.

Affixed Goods: Entinostat (MS-275) , Trichostatin A (TSA)

Akt Inhibitor

MK-2206 2HCl

MK-2206 2HCl is actually a highly a number of inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, correspondingly no inhibitory actions against 250 other protein kinases noticed. Cycle 2.

Associated Merchandise: AZD5363 , GDC-0068

Raf Inhibitor


Vemurafenib (PLX4032, RG7204) is truly a particular and powerful inhibitor of B-RafV600E with IC50 of 31 nM.

Important Goods: Sorafenib Tosylate , PLX-4720

Goods and services Catalog

Product Range

32 varieties of aspect libraries for major throughput analyzing and information confirmation.

Investigation Locations



JAK/STAT Signaling

Tyrosine Kinase/Adaptors

PI3K/Akt/mTOR Signaling

MAPK Signaling





DNA Cause damage to/DNA Restoration

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Well-appreciated-promoting inhibitors

TargetMol’s well-known-marketing and advertising inhibitors for your personalized assortment.

1. Vemurafenib

Vemurafenib (PLX4032, RG7204) is truly a groundbreaking and strong inhibitor of B-RafV600E with IC50 of 31 nM.

2. Olaparib

Olaparib (AZD2281, KU0059436) is truly a fussy inhibitor of PARP1/2 with IC50 of 5 nM/1 nM, 300-conditions less effective against tankyrase-1. Time 3.

3. Rapamycin

Rapamycin (Sirolimus, AY-22989, WY-090217) is actually a distinct mTOR inhibitor with IC50 of ~.1 nM.

4. Ibrutinib (PCI-32765)

Ibrutinib (PCI-32765) could be a potent and highly choosy Brutons tyrosine kinase (Btk) inhibitor with IC50 of .5 nM, modestly highly effective to Bmx, CSK, FGR, BRK, HCK, significantly less successful to EGFR, Confident, ErbB2, JAK3, and others.

5.  Trametinib

 Trametinib (GSK1120212) might be a highly a number of and powerful MEK1/2 inhibitor with IC50 of .92 nM/1.8 nM, no inhibition in the kinase actions of c-Raf, B-Raf, ERK1/2.

TargetMol is headquartered in Boston, Massachusetts. Our significant products are molecular libraries and inhibitors, which includes over 4000 bioactive factors. Our components bring mobile sending transduction tests, cellphone inducing inspections, product or service repositioning, and advantageous managing assessments.

Goal Molecule Corp.

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Natural Compound Catalogue

Our Natural Compound Library, containing as much as 623 substances.

Organic merchandise still continues to be the finest types of drugs and substance sales opportunities these days. They represent the most prosperous supply of innovative molecular scaffolds and chemistry. Nonetheless, normal items hold massive structural and compound diversity which is unsurpassed by any man-made libraries. The invention newest organic items promises considerable advancements not just in chemistry, but in addition, biochemistry and treatment.

Considering that all-natural items are significantly underrepresented in recent modest molecule libraries, In my opinion that TargetMol’s Normal Compounds Library may offer you the good opportunity to deliver far more unpredicted breakthroughs.

Explanations & advantages:

1. Involves 623 normal compounds which can be used as great throughput screening(HTS) and content material testing(HCS)

2. NMR and HPLC validated to make sure high purity and high quality

3. Merchandise composition involves: Alkaloids, Flavonoids, Glycosides, Phenols, Phenylpropanoids, Quinones, Saccharides, Steroids, and Terpenoids, and many others

4. Medicinally active, and cell permeable

Goal Molecule Corp

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Federal substance administration-approved drug library

Presently, you will find no certified vaccines or distinctive remedies to avoid or handle Zika illness (ZIKV) contaminants. On 28 July, there is clearly an analysis introduced on Mobile phone, which interrogated a collection of FDA-approved medications with regard to their capacity to prohibit condition of human being HuH-7 tissues with a newly divided ZIKV stress. 774 Approved by the fda medicines were actually screened for anti–Zika malware action and also over 20 resources demonstrated contra–Zika virus process. Picked substances had been also validated in human neural can come tissues and primary amnion tissue.

This study implies that tests licensed drugs may lead a simple idea of your respective potential contra –computer virus or contra–illness work in out-of-date prescription drugs. It may increase this process to formulate treatment solution strategies. However, only 774 drugs were utilised in this analysis.

We at TargetMol are offering the FDA-approved Drug Library  with 1068 medications integrated, which may provide a lot more opportunities to discover prescription medications centering on new successful internet sites. Furthermore, we are also servicing one of the most substantial collection of Approved Drug Library (1700 drugs) which will definitely boosted to learn new use for more mature medications. Every one of the libraries will be the profitable source of information in your own substance repositioning attached examination.

FDA-approved Drug Library Outline:

1. A distinctive selection of 1068 FDA-approved Drug Library  for top throughput analyzing (HTS) and written content verification (HCS)

2. All components have been authorized by Meals and substance management

3. Which include a number of area, by way of example oncology, cardiology, contra –inflamation, immunology, neuropsychiatry, etc

Approved Drug Library Product descriptions:

1. A special selection of 1700 acknowledged drugs for top throughput testing (HTS) and content articles testing (HCS)

2. All compounds have been licensed by the FDA, CFDA, or emea etc. with identified pharmacology and toxicology information and facts

3. Such as numerous discipline, which includes oncology, cardiology, anti–inflamation, immunology, neuropsychiatry, or anything else

Objective Molecule Corp

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Evaluating Libraries and inhibitors

Lately, we are changing several new inhibitors inside our product range, We have preferred 5 of those as following. TargetMol is devoted to adding much more modest molecular inhibitors in stock and provide a lot more selections for your quest.

1. DAA1106

DAA1106 is actually a effective and particular ligand for peripheral benzodiazepine receptor (PBR), as being a effective and discerning agonist at the peripheral benzodiazepine receptor. ( code)

2. Taprenepag

Taprenepag (CP-544326) is really a strong and selective prostaglandin E2 receptor agonist (EC50 = 2.8 nM).

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3.  Briciclib

 Briciclib is actually a small molecule that inhibits cyclin D1 accumulation in cancer cells. ( coding)

4. R112

R112 is undoubtedly an ATP-competitive inhibitor of Syk kinase using a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.

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5. JNJ-42041935

JNJ-42041935 can be a potent (pKi = 7.3-7.9), 2-oxoglutarate aggressive, reversible, and discerning inhibitor of PHD digestive enzymes.

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In order to learn more about our inhibitors, kindly visit:

TargetMol is headquartered in Boston, Massachusetts. Our central items are molecular libraries and inhibitors, that include over 4000 bioactive materials. Our substances can be used for mobile transmission transduction tests, mobile inducing experiments, drug repositioning, and positive management tests.

Remember to just response this email when you are fascinated or possess further questions.

Goal Molecule Corp.

Tackle: 1 Boston Spot, Collection 2600, Boston, Massachusetts, 02108

Evaluating Libraries and inhibitors

Recently, our business is updating several new inhibitors within our goods collection, I actually have selected 5 of the as adhering to. TargetMol is dedicated to adding a lot more modest molecular inhibitors in store and offer considerably more alternatives for your quest.

1. DAA1106

DAA1106 is in reality a potent and picky ligand for peripheral benzodiazepine receptor (PBR), becoming a effective and distinct agonist in the peripheral benzodiazepine receptor. ( html coding)

2. Taprenepag

Taprenepag (CP-544326) is actually a effective and discerning prostaglandin E2 receptor agonist (EC50 = 2.8 nM).

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3. Briciclib

Briciclib is really a tiny molecule that inhibits cyclin D1 deposition in many forms of cancer tissue. ( code computer code)

4. R112

R112 is definitely an ATP-competing inhibitor of Syk kinase having a Ki of 96 nM. R112 inhibits Syk kinase physical exercise by getting an IC50 of 226 nM.

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5. JNJ-42041935

JNJ-42041935 is truly a powerful (pKi = 7.3-7.9), 2-oxoglutarate competing, reversible, and fussy inhibitor of PHD nutrition.

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If you would like continue reading about our inhibitors, look at: coding

TargetMol is headquartered in Boston, Massachusetts. Our core items are molecular libraries and inhibitors, like over 4000 bioactive substances. Our compounds can be utilized mobile indicate transduction tests, mobile inducing tests, treatment repositioning, and beneficial managing checks.

Ensure you just answer this email in case you are fascinated or have a lot more problems.

Focus on Molecule Corp.

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GPCR component collection

GPCR Compound Library receptors (GPCRs) mediate lots of crucial physiologic characteristics and they are viewed as among the very best curing is focused on for that wide range of problems. The style and program of great-throughput GPCR assays which allow the charge-successful screening of substantial product libraries to determine unique chemical prospective customers are crucial in early treatments development.

TargetMol is providing a thorough assortment of 356 elements targeted GPCRs. It might be a highly effective product for your personal medicine verification evaluation looking for at GPCR concentrates on.

Product descriptions & good aspects

1. A distinctive range of 356 resources for GPCR Particular drug evaluating

2. The GPCR Compound Library involves tiny substances connected with receptors such as 5-HT Receptor, Dopamine Receptor, Opioid Receptor, Adrenergic Receptors, Cannabinoid Receptor, mGluR, and ETA-receptor and so forth

3. It is in reality calculated about 200 so-named orphan GPCRs are functionally different, due to this, use of our GPCR Small Molecule Ingredient Collection for evaluating the functionally unfamiliar GPCRs may produce potentially new GPCR-based medication prospects

4. Structurally varied, medicinally lively, and cell phone permeable

Aim Molecule Corp.

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Inhibitor Library

Inhibitor Library, including 109 substances connected PI3K/Akt/mTOR pathway.

The PI3K/Akt and mTOR signaling pathways are two paths crucial to many elements of cellular growth and survival, in physiologic as well as in pathological circumstances. The activation of the PI3K/Akt/mTOR pathway results in a significant disturbance of charge of cellular expansion and emergency, which ultimately results in a aggressive growth benefit, metastatic skills, angiogenesis, and treatment method level of resistance. Novel substances aimed towards PI3K/Akt/mTOR guarantee further more development of the results achieved thus far through better selectivity advertising strength, as well as to combinability along with other therapeutic techniques.

As a result, we at TargetMol are setting up the selection of 109 substances which can be completely ready to use with your associated pathway or medicine verification research.

Descriptions & pros:

1. An original collection of 109 bioactive materials related to PI3K/Akt/mTOR

2. A highly effective device to learn of mobile phone/tumor cellular growth, proliferation, apoptosis

3. Focuses on involve: Akt, AMPK, mTOR, PI3K, ATR/ATM and so forth

4. Medicinally lively, and cell permeable

Focus on Molecule Corp.

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2600 Boston, MA 02108

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Kinase Inhibitor Library

Kinase Inhibitor Library, that contains approximately 481 kinase inhibitors.

Healthy healthy proteins kinases conduct important features in regulating most cell capabilities–proliferation/cellphone program, mobile metabolic rate, enduring/apoptosis, DNA damage routine maintenance, cell phone motility, and many more. Meanwhile, signaling internet sites that use phosphorylation to modulate focus on actions have shown to be critically involved with every factor of mobile function, as well as in cancer, the unusual activation of proteins phosphorylation is normally either a motorist or quick consequence of the health problems.

Presented this chance for restorative assistance, we have seen significant hard work in developing pharmacological devices to protect against protein phosphorylation and interrogate signaling.

TargetMol’s kinase inhibitor assortment consists of 481 supplies concentrating on particular well being proteins kinase, that will be the successful device for the individual linked HTS and HCS research.

Information and facts:

1. An exclusive assortment of 481 types of kinase inhibitors for HTS and HCS

2. Targets entail kinase, such as MAPK, PI3K, JAK, STAT, CDK and MEK, etc.

3. Biological activity and safety is established through preliminary clinical studies and numerous scientific studies

4. Several of these kinase inhibitors have been accredited by FDA

5. Nearly all them would be the ATP contesting inhibitors

6. Structurally diverse, medicinally effective, and mobile permeable

7. In depth features, chemical platform, target, IC50 benefit, activity info, and so on

8. NMR and HPLC validated to be certain substantial wholesomeness

Goal Molecule Corp.

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Anti-infection Compound Library

Anti-infection Compound Library, including 423 contra –infective modest substances.

Despite you require ingredients using the biological activity of prescription antibiotic, anti-bacterial, anti-fungal, antiviral, contra–CMV, or antiparasitic, and so forth., our materials local library could satisfy your requirements.

Product descriptions & pros:

1. A distinctive collection of 423 compounds for HTS and HCS

2. Substances consist of antibacterial, antifungal, anti–CMV, anti-HIV, anti-influenza computer virus, and many others

3. Some contra–illness drugs are already accepted by Federal drug administration

4. Biological activity and protection continues to be confirmed through preliminary scientific studies and clinical studies

5. Structurally diverse, medicinally productive, and mobile permeable

Focus on Molecule Corp.

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2600 Boston, MA 02108