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Venetoclax

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (2) Autophagy (3) Bcl-2 Family (5) Drug Metabolite (1) E3 Ligase Ligand-Linker Conjugates (1) HDAC (1) PI3K (1) PROTACs (1)
By Research Areas:	Cancer (9)

Inhibitors & Agonists

Screening Libraries

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15531

*Venetoclax* 145+ Cited Publications 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-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 Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].

HY-142209

ABBV-167	Bcl-2 Family	Cancer
ABBV-167 is a phosphate proagent of the BCL-2 inhibitor venetoclax.

HY-163677

ARM165	PROTACs PI3K Akt	Cancer
ARM165 is a heterobifunctional molecule. ARM165 degrades the PIK3CG proteins, inhibits PI3Kγ-Akt signaling pathway, and thus exhibits antileukemia efficacy. ARM165 inhibits proliferations of AML cells, with IC₅₀ <1 μM. (Pink: ligand for target protein PI3Kγ inhibitor AZ2 (HY-111570); Black: linker; Blue: ligand for E3 ligase Pomalidomide (HY-10984))

HY-15531R

Venetoclax (Standard)	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-133772

Venetoclax N-oxide	Drug Metabolite	Others
Venetoclax N-oxide is an impurity of Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM .

HY-162769

HDAC3-IN-5	HDAC Apoptosis	Cancer
HDAC3-IN-5 (9c) is a HDAC3 selective inhibitor, with IC₅₀ values of 4.2 nM, 1629 nM and 298.2 nM for HDAC3, HDAC2, HDAC1, respectively. HDAC3-IN-5 (9c) can effectively induce apoptosisin MV4-11 cells in vitro and reduce the expression of anti-apoptotic proteins, the development of HDAC3 selective inhibitors may serve as a potential lead compound to reverse Venetoclax resistance .

HY-162642

Bfl-1-IN-3	Bcl-2 Family	Cancer
Bfl-1-IN-3 (Compound 56) is a selective, competitive inhibitor for Bfl-1 on BID binding site with K_i of 105 nM. Bfl-1-IN-3 inhibits the proliferation of cell pfeiffer and MV4-11, with IC₅₀ of 6.92 μM and 12.6 μM. Bfl-1-IN-3 induces apoptosis in pfeiffer cells. Bfl-1-IN-3 overcomes Venetoclax (HY-15531) resistance at the cellular level, and shows synergistically enhanced anti-tumor activity with Venetoclax .

HY-154971

Ara-SH	Apoptosis	Cancer
Ara-SH is a Cytarabine mercaptopropionic acid-substituted derivative. Ara-SH is used as the trigger to fabricate a smart Cytarabine and Venetoclax-coloaded nanoparticle (AV-NP) through self-assembly. Ara-SH exhibits remarkable synergistic antileukemia effects in vitro and in vivo .

HY-163678

Pomalidomide-CO-C7-NH-CO-C3-COOH	E3 Ligase Ligand-Linker Conjugates	Cancer
Pomalidomide-CO-C7-NH-CO-C3-COOH is a conjugate of a ligand for E3 ligase and a linker. Pomalidomide-CO-C7-NH-CO-C3-COOH can be used for synthesis of PROTAC degrader ARM165 (HY-163677) .

Cat. No.	Product Name

HY-L187

Structurally Diverse Fragment Library	2,323 compounds
Fragment-based drug development (FBDD) is a strategy for drug discovery that can be applied both academically and commercially to enhance the identification of some non-drug targets. Fragment-based drug development has identified low molecular weight molecules (<300 Da) capable of binding to related macromolecules. These fragments can cover a wide chemical space and are easy to optimize later. Currently, several fragment-based drugs have entered clinical trials, of which two drugs, Vemurafenib and Venetoclax, have been approved for marketing. Based on Tanimoto coefficient, MCE uses similarity algorithm to carefully select 2,323 high-structurally diverse 'RO3' compliant fragment molecules from large-scale fragment molecules, which can be applied to fragment based drug development.

Structurally Diverse Fragment Library

2,323 compounds

Fragment-based drug development (FBDD) is a strategy for drug discovery that can be applied both academically and commercially to enhance the identification of some non-drug targets. Fragment-based drug development has identified low molecular weight molecules (<300 Da) capable of binding to related macromolecules. These fragments can cover a wide chemical space and are easy to optimize later. Currently, several fragment-based drugs have entered clinical trials, of which two drugs, Vemurafenib and Venetoclax, have been approved for marketing.

Based on Tanimoto coefficient, MCE uses similarity algorithm to carefully select 2,323 high-structurally diverse 'RO3' compliant fragment molecules from large-scale fragment molecules, which can be applied to fragment based drug development.

HY-L032

Fragment Library	22,824 compounds
Fragment-based drug discovery (FBDD) is well suited for discovering both drug leads and chemical probes of protein function; it can cover broad swaths of chemical space and allows the use of creative chemistry. Fragment-based drug discovery is well-established in industry and has resulted in a variety of drugs entering clinical trials, with two, vemurafenib and venetoclax, already approved. FBDD also has key attractions for academia. Notably, it is able to tackle difficult or novel targets for which no chemical matter may be found in existing HTS collections. MCE designs a unique collection of 22,824 fragment compounds, all of which obey a heuristic rule called the “Rule of Three (RO3) ”, in which molecular weight ≤300 Da, the number of hydrogen bond donors (H-donors) ≤3, the number of hydrogen bond acceptors (H-acceptors) is ≤3 and cLogP is ≤3. This library is an important source of lead-like drugs.

Fragment Library

22,824 compounds

Fragment-based drug discovery (FBDD) is well suited for discovering both drug leads and chemical probes of protein function; it can cover broad swaths of chemical space and allows the use of creative chemistry. Fragment-based drug discovery is well-established in industry and has resulted in a variety of drugs entering clinical trials, with two, vemurafenib and venetoclax, already approved. FBDD also has key attractions for academia. Notably, it is able to tackle difficult or novel targets for which no chemical matter may be found in existing HTS collections.

MCE designs a unique collection of 22,824 fragment compounds, all of which obey a heuristic rule called the “Rule of Three (RO3) ”, in which molecular weight ≤300 Da, the number of hydrogen bond donors (H-donors) ≤3, the number of hydrogen bond acceptors (H-acceptors) is ≤3 and cLogP is ≤3. This library is an important source of lead-like drugs.

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 Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].

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