Search Result

Results for "

highly bioavailable

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (1) Apoptosis (20) ATM/ATR (1) Autophagy (16) Bacterial (2) Bcl-2 Family (4) Btk (2) c-Met/HGFR (3) Casein Kinase (5) CCR (1) CDK (3) CGRP Receptor (2) Checkpoint Kinase (Chk) (1) Complement System (1) CXCR (1) Drug Metabolite (1) E1/E2/E3 Enzyme (1) Elastase (3) Epigenetic Reader Domain (4) Fatty Acid Synthase (FASN) (1) Ferroptosis (2) FGFR (2) FLT3 (1) GSK-3 (2) HBV (1) HCV (3) HCV Protease (3) Histone Methyltransferase (1) HIV (7) HIV Integrase (5) HSP (2) IAP (1) IFNAR (1) Interleukin Related (1) Isotope-Labeled Compounds (6) JAK (6) LPL Receptor (1) mAChR (1) MAP4K (1) MDM-2/p53 (1) mGluR (5) Microtubule/Tubulin (3) Mps1 (3) NF-κB (1) NOD-like Receptor (NLR) (1) P2X Receptor (1) PARP (9) PERK (1) Phosphodiesterase (PDE) (1) PI3K (6) Pim (2) PROTACs (1) Proteasome (1) PTHR (1) Raf (1) Reference Standards (19) SARS-CoV (3) Sodium Channel (1) Tau Protein (1) Toll-like Receptor (TLR) (1) VEGFR (1) γ-secretase (2)
By Research Areas:	Cancer (58) Cardiovascular Disease (3) Endocrinology (1) Infection (12) Inflammation/Immunology (17) Metabolic Disease (3) Neurological Disease (14)

By Targets:

Androgen Receptor (1)

Apoptosis (20)

ATM/ATR (1)

Autophagy (16)

Bacterial (2)

Bcl-2 Family (4)

Btk (2)

c-Met/HGFR (3)

Casein Kinase (5)

CCR (1)

CDK (3)

CGRP Receptor (2)

Checkpoint Kinase (Chk) (1)

Complement System (1)

CXCR (1)

Drug Metabolite (1)

E1/E2/E3 Enzyme (1)

Elastase (3)

Epigenetic Reader Domain (4)

Fatty Acid Synthase (FASN) (1)

Ferroptosis (2)

FGFR (2)

FLT3 (1)

GSK-3 (2)

HBV (1)

HCV (3)

HCV Protease (3)

Histone Methyltransferase (1)

HIV (7)

HIV Integrase (5)

HSP (2)

IAP (1)

IFNAR (1)

Interleukin Related (1)

Isotope-Labeled Compounds (6)

JAK (6)

LPL Receptor (1)

mAChR (1)

MAP4K (1)

MDM-2/p53 (1)

mGluR (5)

Microtubule/Tubulin (3)

Mps1 (3)

NF-κB (1)

NOD-like Receptor (NLR) (1)

P2X Receptor (1)

PARP (9)

PERK (1)

Phosphodiesterase (PDE) (1)

PI3K (6)

Pim (2)

PROTACs (1)

Proteasome (1)

PTHR (1)

Raf (1)

Reference Standards (19)

SARS-CoV (3)

Sodium Channel (1)

Tau Protein (1)

Toll-like Receptor (TLR) (1)

VEGFR (1)

γ-secretase (2)

By Research Areas:

Cancer (58)

Cardiovascular Disease (3)

Endocrinology (1)

Infection (12)

Inflammation/Immunology (17)

Metabolic Disease (3)

Neurological Disease (14)

102

Inhibitors & Agonists

Screening Libraries

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15531

Venetoclax Maximum Cited Publications 227 Publications Verification ABT-199; GDC-0199; RG7601	Bcl-2 Family Autophagy	Cancer
Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a K_i of less than 0.01 nM. Venetoclax induces autophagy .

HY-10619

Niraparib 80+ Cited Publications MK-4827	PARP Apoptosis	Cancer
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .

HY-50855

Silmitasertib 55+ Cited Publications CX-4945	Casein Kinase Autophagy	Cancer
Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC₅₀ values of 1 nM against CK2α and CK2α'.

HY-100818

Futibatinib 5+ Cited Publications TAS-120	FGFR	Cancer
Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC₅₀s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC₅₀s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .

HY-109566

AZD1390 5+ Cited Publications	ATM/ATR	Inflammation/Immunology Cancer
AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC₅₀ of 0.78 nM in cell .

HY-13026

Idelalisib 55+ Cited Publications CAL-101; GS-1101	PI3K Autophagy	Cancer
Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC₅₀ of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.

HY-15785

Pimitespib 5+ Cited Publications TAS-116	HSP	Cancer
Pimitespib (TAS-116) is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (K_is of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94 . Pimitespib demonstrates less ocular toxicity .

HY-13238

Dolutegravir 30+ Cited Publications S/GSK1349572	HIV Integrase HIV	Infection
Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-15959

Savolitinib 5+ Cited Publications Volitinib; HMPL-504; AZD-6094	c-Met/HGFR	Cancer
Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC₅₀s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity .

HY-15604

AZD1208 20+ Cited Publications	Pim Autophagy Apoptosis	Cancer
AZD1208 is an orally bioavailable, highly selective PIM kinases inhibitor .

HY-139567

Afimetoran 1 Publications Verification BMS-986256	Toll-like Receptor (TLR) NF-κB Apoptosis	Inflammation/Immunology
Afimetoran (BMS-986256) is an orally active, selective, and highly bioavailable TLR7/8 antagonist. Afimetoran (BMS-986256) can inhibit TLR7/8 activation of the NF-κB pathway and reverse TLR7 mediated resistance to steroid induced apoptosis in plasma cell like dendritic cells (pDCs). Afimetoran (BMS-986256) can be used for research on inflammation and autoimmune diseases (systemic lupus erythematosus) .

HY-16925

MI-503 5+ Cited Publications	Epigenetic Reader Domain	Cancer
MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

HY-10237

Boceprevir 30+ Cited Publications EBP 520; SCH 503034	HCV Protease HCV SARS-CoV	Infection
Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a K_i of 14 nM in both enzyme assay and an EC₉₀ of 350 nM in cell-based replicon assay . Boceprevir inhibits SARS-CoV-2 3CL ^pro activity .

HY-50855B

Silmitasertib sodium salt 55+ Cited Publications CX-4945 sodium salt	Casein Kinase Autophagy	Cancer
Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC₅₀ values of 1 nM against CK2α and CK2α'.

HY-101340

Luvixasertib 5+ Cited Publications CFI-402257	Mps1	Cancer
CFI-402257 is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC₅₀ of 1.7 nM for TTK in vitro. CFI-402257 has anti-cancer activity .

HY-117650A

RG7834 5+ Cited Publications RO 7020322; (S)-RO0321	HBV	Infection
RG7834 (RO 7020322) is a highly selective and orally bioavailable HBV inhibitor, potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC₅₀s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells .

HY-15531S

Venetoclax-d8 ABT-199-d₈; GDC-0199-d₈; RG7601-d₈	Bcl-2 Family Autophagy	Cancer
Venetoclax-d₈ is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a K_i of less than 0.01 nM. Venetoclax induces autophagy .

HY-120062

TVB-3664 5 Publications Verification	Fatty Acid Synthase (FASN)	Cancer
TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC₅₀ values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression .

HY-13270

ABT-751 E7010	Microtubule/Tubulin Autophagy Apoptosis	Cancer
ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .

HY-18658

Siremadlin 10+ Cited Publications NVP-HDM201; HDM201	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
Siremadlin (NVP-HDM201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.

HY-10619B

Niraparib tosylate 80+ Cited Publications MK-4827 tosylate	PARP Apoptosis	Cancer
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC₅₀ of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .

HY-10619A

Niraparib hydrochloride 80+ Cited Publications MK-4827 hydrochloride	PARP Apoptosis	Cancer
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .

HY-13238A

Dolutegravir sodium 30+ Cited Publications S/GSK1349572 sodium	HIV Integrase HIV	Infection
Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-101800

Senexin B 2 Publications Verification SNX2-1-165; BCD-115	CDK	Cancer
Senexin B (SNX2-1-165; BCD-115) is a potent, highly water-soluble and bioavailable CDK8/19 inhibitor, with K_ds of 140 nM for CDK8 and 80 nM for CDK19.

HY-10619E

Niraparib tosylate hydrate 80+ Cited Publications MK-4827 tosylate hydrate	PARP Apoptosis	Cancer
Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .

HY-15531R

Venetoclax (Standard) ABT-199 (Standard); GDC-0199 (Standard); RG7601 (Standard)	Reference Standards Bcl-2 Family Autophagy	Cancer
Venetoclax (Standard) is the analytical standard of Venetoclax. This product is intended for research and analytical applications. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a K_i of less than 0.01 nM. Venetoclax induces autophagy .

HY-13208

Xevinapant hydrochloride 10+ Cited Publications AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride	IAP Apoptosis	Cancer
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with K_is of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .

HY-W698249

Ferrous gluconate	Ferroptosis Bacterial	Cardiovascular Disease Infection
Ferrous gluconate is a highly water-soluble iron-containing agent with high bioavailability and bactericidal activity. As a non-heme iron, Ferrous gluconate is used for meat product fortification and improvement of iron deficiency anemia. Ferrous gluconate induces ferroptosis in E. coli through Fe ²⁺ infiltration, reactive oxygen species burst, lipid peroxidation and direct interaction with DNA. Ferrous gluconate also downregulates the SOS responsive transcriptional repressor LexA. In addition, Ferrous gluconate regulates multiple key pathways in E. coli such as fatty acid metabolism, iron-sulfur cluster assembly and pyruvate metabolism, and is applied in studies related to E. coli infection and iron deficiency anemia .

HY-19809

MI-463 2 Publications Verification	Epigenetic Reader Domain	Cancer
MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

HY-116000

Glumetinib 2 Publications Verification Gumarontinib; SCC244	c-Met/HGFR	Cancer
Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC₅₀ of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity .

HY-128570

FD-IN-1	Complement System	Inflammation/Immunology
FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC₅₀ of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC₅₀s of 7.7 and 6.5 µM, respectively .

HY-176533

S1PR5-IN-1	LPL Receptor	Neurological Disease
S1PR5-IN-1 (Compound 7a) is a highly selective S1PR5 antagonist and orally bioavailable inhibitor with a human S1PR5 IC₅₀ of 85.4 nM and human S1PR5 K_d of 2.173 nM.S1PR5-IN-1 binds to S1PR5 and inhibits natural killer cell migration toward sphingosine-1-phosphate.S1PR5-IN-1 can be used for the research of multiple sclerosis .

HY-18175

CCT244747 5 Publications Verification	Checkpoint Kinase (Chk)	Cancer
CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC₅₀ of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC₅₀ of 29 nM.

HY-101340A

Luvixasertib hydrochloride 5+ Cited Publications CFI-402257 hydrochloride	Mps1	Cancer
CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC₅₀ of 1.7 nM for TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity .

HY-111457A

BAY-678 1 Publications Verification	Elastase	Inflammation/Immunology
BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC₅₀ of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

HY-19631A

Ilginatinib 1 Publications Verification NS-018	JAK	Cancer
Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC₅₀ of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC₅₀, 33 nM), JAK3 (IC₅₀, 39 nM), and Tyk2 (IC₅₀, 22 nM).

HY-111790

M3258 5 Publications Verification	Proteasome Apoptosis	Cancer
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC₅₀=3.6 nM) and cellular (IC₅₀=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .

HY-141711

VU6028418	mAChR	Neurological Disease
VU6028418 is a potent, highly selective and orally bioavailable M₄ mAChR antagonist with an IC₅₀ of 4.1 nM against hM₄ .

HY-107457

AZD-8529 1 Publications Verification	mGluR	Neurological Disease
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC₅₀ of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

HY-19631B

Ilginatinib hydrochloride 1 Publications Verification NS-018 hydrochloride	JAK	Cancer
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC₅₀ of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC₅₀, 33 nM), JAK3 (IC₅₀, 39 nM), and Tyk2 (IC₅₀, 22 nM).

HY-19631

Ilginatinib maleate 1 Publications Verification NS-018 maleate	JAK	Cancer
Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC₅₀ of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC₅₀, 33 nM), JAK3 (IC₅₀, 39 nM), and Tyk2 (IC₅₀, 22 nM).

HY-100886

BAY1082439	PI3K Apoptosis	Cancer
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth .

HY-132292

ARD-2128	PROTACs Androgen Receptor	Cancer
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer .

HY-10302

MK-3207 Hydrochloride 5 Publications Verification	CGRP Receptor	Neurological Disease
MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC₅₀ of 0.12 nM and K_i of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.

HY-116804

ZLD1039	Histone Methyltransferase	Cancer
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC₅₀ values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .

HY-117482

BPN-15606	γ-secretase	Neurological Disease
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC₅₀ values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance .

HY-138563

GSK973	Epigenetic Reader Domain	Cancer
GSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC₅₀ of 7.8 and a pK_d of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC₅₀=7.4~7.8; pK_d=8.3~8.5) .

HY-125879

DS08210767	PTHR	Metabolic Disease Endocrinology
DS08210767 is a highly potent, orally bioavailable PTHR1 antagonist with IC₅₀ of 90 nM .

HY-10096

TCS2002	GSK-3	Neurological Disease
TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC₅₀ of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease .

HY-142160

GNE-9815	Raf	Cancer
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits K_i values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers .

Cat. No.	Product Name

HY-L901

50K Diversity Library

50,000 compounds

MCE 50K Diversity Library consists of 50,000 lead-like compounds with multiple characteristics such as calculated good solubility (-3.2 < logP < 5), oral bioavailability (RotB <= 10), drug transportability (PSA < 120). These compounds were selected by dissimilarity search with an average Tanimoto Coefficient of 0.52. There are 36,857 unique scaffolds and each scaffold 1 to 7 compounds. What’s more, compounds with the same scaffold have as many functional groups as possible, which make abundant chemical spaces. This exceptionally diverse library is highly recommended for random screening against new as well as popular targets based its novel, diverse scaffolds, abundant chemical spaces and the convenience for subsequent modification.

HY-L929

Fragment Library with Good Solubility

2,527 compounds

In drug discovery and development (R&D) area, target binding and druggability optimization are core processes. Among these attributes, high solubility is critical for a compound to achieve druggability, as it directly impacts the progress of drug R&D. Superior solubility ensures the rapid dissolution and uniform distribution of drug molecules in vivo, thereby enhancing bioavailability and effectively mitigating issues such as suboptimal efficacy, increased dosage requirements, or exacerbated toxic and side effects arising from insufficient solubility.

From the perspective of medicinal chemistry, high-solubility drug fragments serve as high-quality "molecular building blocks". Based on these fragments, lead compounds with potential druggability can be rapidly screened out, which significantly shortens the drug R&D cycle and reduces R&D costs. Meanwhile, the high-solubility drug fragment library can provide diverse options for drug development in different therapeutic areas, offer solutions for the solubility defects of existing clinical drugs, and facilitate the development of novel, highly effective targeted drugs with higher bioavailability and better safety profiles.

MCE has collected and compiled 2,527 experimentally validated small-molecule fragments with high solubility. These fragments can be directly used for drug molecular design, providing high-quality pre-validated solubility fragments that significantly improve the efficiency of lead compound screening and accelerate the progress of drug R&D.

HY-L214

Liposome Library

190 compounds

Liposomes are spherical or multilayered spherical vesicles formed by the self-assembly of diacyl chain phospholipids (lipid bilayers) in aqueous solutions, which can be made from natural or synthetic phospholipids and exhibit good biocompatibility and low toxicity. They can serve as delivery carriers for various bioactive substances (such as drugs, proteins, nucleic acids, etc.) and are widely used in biomedical and chemical research. The main advantages of liposomes include 1) Protective effect: Their bilayer structure can protect encapsulated molecules from enzymatic degradation, oxidation, and other influences, extending stability and activity; 2) Active targeting: Surface modifications enable active targeting, enhancing the concentration of drugs or molecules in specific tissues or cells; 3) Customizability: The composition and structure of liposomes can be adjusted according to needs, such as altering phospholipid types or adding targeting ligands. These properties make liposomes highly valuable in developing novel drug delivery systems, serving as nucleic acid carriers for gene transfection, studying cellular uptake mechanisms and drug release kinetics, as well as developing functional food additives to improve the bioavailability of nutritional components.

MCE contains 190 liposome compounds, which is a good tool for lipidomic-related studies.

Cat. No.	Product Name	Chemical Structure

HY-15531S

Venetoclax-d8
Venetoclax-d₈ is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a K_i of less than 0.01 nM. Venetoclax induces autophagy .

HY-13026S

Idelalisib-d5
Idelalisib-d₅ is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ inhibitor .

HY-15531S1

Venetoclax-d6
Venetoclax-d₆ (ABT-199-d₆) is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a K_i of less than 0.01 nM. Venetoclax induces autophagy .

HY-13238S1

Dolutegravir-d3

Dolutegravir-d₃ is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-13238S2

Dolutegravir-d5

Dolutegravir-d₅ is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-10237S

Boceprevir-d9
Boceprevir-d₉ is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a K_i of 14 nM in both enzyme assay and an EC₉₀ of 350 nM in cell-based replicon assay . Boceprevir inhibits SARS-CoV-2 3CLpro activity .

HY-W759435

Niraparib-d5
Niraparib-d₅ (MK-4827-d₅) is the deuterium labeled Niraparib (HY-10619). Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .

HY-166594S

Deucravacitinib-13C,d3

Deucravacitinib- ¹³C,d₃ is the ¹³C- and deuterium labeled Deucravacitinib. Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC₅₀=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: