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AB218114

ABT-263, Bcl-2 family protein inhibitor

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MW 974.6 Da, Purity >98%. Potent, small molecule Bcl-2 family protein inhibitor (Ki's of <1 nM for Bcl-2, Bcl-XL and Bcl-w). Orally bioavailable. Displays anticancer properties. Selectively binds to apoptosis suppressor proteins Bcl-2, Bcl-XL, and Bcl-w and disrupts Bcl-2/Bcl-XL interactions with pro-death proteins, leading to the initiation of apoptosis. Induces Bax translocation, cytochrome c release, and subsequent apoptosis.

Key facts

CAS number

923564-51-6

Purity

>98%

Form

Solid

form

Molecular weight

974.6 Da

Molecular formula

C<sub>4</sub><sub>7</sub>H<sub>5</sub><sub>5</sub>ClF<sub>3</sub>N<sub>5</sub>O<sub>6</sub>S<sub>3</sub>

PubChem

24978538

Nature

Synthetic

Solubility

Soluble in DMSO to 50 mM

Biochemical name

Navitoclax

Biological description

Potent, small molecule Bcl-2 family protein inhibitor (Ki's of <1 nM for Bcl-2, Bcl-XL and Bcl-w). Orally bioavailable. Displays anticancer properties. Selectively binds to apoptosis suppressor proteins Bcl-2, Bcl-XL, and Bcl-w and disrupts Bcl-2/Bcl-XL interactions with pro-death proteins, leading to the initiation of apoptosis. Induces Bax translocation, cytochrome c release, and subsequent apoptosis.

Canonical smiles

CC1(CCC(=C(C1)CN2CCN(CC2)C3=CC=C(C=C3)C(=O)NS(=O)(=O)C4=CC(=C(C=C4)NC(CCN5CCOCC5)CSC6=CC=CC=C6)S(=O)(=O)C(F)(F)F)C7=CC=C(C=C7)Cl)C

Isomeric smiles

CC1(CCC(=C(C1)CN2CCN(CC2)C3=CC=C(C=C3)C(=O)NS(=O)(=O)C4=CC(=C(C=C4)N[C@H](CCN5CCOCC5)CSC6=CC=CC=C6)S(=O)(=O)C(F)(F)F)C7=CC=C(C=C7)Cl)C

InChi

InChI=1S/C47H55ClF3N5O6S3/c1-46(2)20-18-42(34-8-12-37(48)13-9-34)36(31-46)32-55-22-24-56(25-23-55)39-14-10-35(11-15-39)45(57)53-65(60,61)41-16-17-43(44(30-41)64(58,59)47(49,50)51)52-38(19-21-54-26-28-62-29-27-54)33-63-40-6-4-3-5-7-40/h3-17,30,38,52H,18-29,31-33H2,1-2H3,(H,53,57)/t38-/m1/s1

InChiKey

JLYAXFNOILIKPP-KXQOOQHDSA-N

IUPAC Name

4-[4-[[2-(4-chlorophenyl)-5,5-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide

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Complementary Products

Biochemicals

AB217298

ABT-199 (Venetoclax), Bcl-2 inhibitor.

Chemical Structure - ABT-199 (Venetoclax), Bcl-2 inhibitor. (AB217298)

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  • 0
Primary Antibodies

AB174316

Anti-LOX antibody [EPR4025]

RabMAb|Recombinant|KO Validated

Flow Cytometry (Intracellular) - Anti-LOX antibody [EPR4025] (AB174316)

  • 4
  • 5
Primary Antibodies

AB227830

Anti-ATF6 antibody [EPR22690-84] - ChIP Grade

BOND RX™ Validated|RabMAb|Advanced Validation|Recombinant|KO Validated

ChIP - Anti-ATF6 antibody [EPR22690-84] - ChIP Grade (AB227830)

  • 5
  • 3
Primary Antibodies

AB32445

Anti-Bad antibody [Y208]

BOND RX™ Validated|20ul selling size|RabMAb|Recombinant|KO Validated

Western blot - Anti-Bad antibody [Y208] (AB32445)

  • 4
  • 13
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Product details

This product is manufactured by BioVision, an Abcam company and was previously called 2467 ABT-263. 2467-25 is the same size as the 25 mg size of ab218114.
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Properties and storage information

Shipped at conditions
Blue Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

The protein known as Bad belongs to the Bcl-2 family and functions in promoting apoptosis. It has a molecular mass of approximately 23 kDa. Bad acts as a pro-apoptotic factor by heterodimerizing with anti-apoptotic proteins like Bcl-XL and Bcl-2 disrupting their protective function. Bad expression mainly occurs in mammalian cells particularly in the cytosol where it remains inactive in its phosphorylated form. DNA Polymerase iota (DNA pol iota) and DNA Polymerase Kappa (PolK) are enzymes responsible for DNA repair and translesion synthesis. Yes1 part of the Src family kinases plays a role in signal transduction. TDP1 (Tyrosyl-DNA phosphodiesterase 1) involves DNA repair specifically in dealing with DNA strand breaks.
Biological function summary

Bad influences the regulation of apoptosis by tethering Bcl-2 and Bcl-XL and freeing Bax or Bak to initiate cell death. DNA Polymerases iota and kappa are involved in error-prone DNA repair mechanisms to allow replication in the presence of DNA damage. Yes1 facilitates several signaling cascades affecting cell growth and differentiation. TDP1 assists in repairing topoisomerase1-mediated DNA breaks. Together these proteins have roles in cellular homeostasis and stress responses functioning individually or as part of molecular complexes.

Pathways

Bad is integral to the intrinsic apoptotic pathway interacting with Bcl-2 and Bcl-XL to modulate programmed cell death. DNA Polymerases iota and kappa participate in the translesion DNA synthesis pathway rectifying DNA damage by bypassing lesions in collaboration with other repair proteins like PCNA. Yes1’s involvement in signaling pathways overlaps with growth factor receptors leading to influences on pathways controlling growth. TDP1 plays a role in the DNA damage response pathway cooperating with other repair proteins to maintain genomic stability.

Bad is associated with various cancers including leukemia due to its ability to regulate apoptosis. Downregulation or mutation can result in resistance to apoptosis contributing to tumorigenesis. Bcl-2 and Bcl-XL often show upregulation in these cancers providing cell survival advantages. DNA polymerases iota and kappa are relevant to cancer development due to their role in increasing mutagenesis under genotoxic stress. DNA repair defects involving TDP1 relate to neurological disorders such as Spinocerebellar Ataxia with Axonal Neuropathy by failing to appropriately repair DNA breaks. Yes1 impacts cancer progression through dysregulation of growth signal transduction aligning it with oncogenic pathways and potentially interacting with other kinases.
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Product protocols

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Product promise

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