Cat. No.: HY-151966

TD1092

Name: TD1092
Brand: MedChemExpress
SKU: HY-151966
Price: 340.00 USD
Availability: InStock
Rating: 5 (1 reviews)

고객리뷰

Based on 1 Customer Validation

TD1092 is a pan-inhibitor of apoptosis protein (IAP) PROTAC degrader that targets cIAP1, cIAP2, and XIAP for degradation. TD1092 induces cell apoptosis by activating caspase. TD1092 inhibits the NF-κB signaling pathway induced by TNFα. TD1092 suppresses TNFα-induced epithelial-mesenchymal transition, cancer cell migration, and invasion. TD1092 is suitable for research on breast cancer, ovarian cancer, melanoma, and inflammation-related diseases.
(Pink: cIAP1 and cIAP2 and XIAP ligand (HY-135997); Blue: Ligands for E3 Ligase ligand (HY-14658); Black: linker).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.23%
CAS No.: 3037417-26-5
화학식: C₅₅H₇₀N₈O₉
분자량:987.19

보관:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

TD1092 Chemical Structure

CAS No.: 3037417-26-5

사이즈

가격

재고

수량

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

HY-115865
XIAP degrader-1

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

TD1092 is a pan-inhibitor of apoptosis protein (IAP) PROTAC degrader that targets cIAP1, cIAP2, and XIAP for degradation. TD1092 induces cell apoptosis by activating caspase. TD1092 inhibits the NF-κB signaling pathway induced by TNFα. TD1092 suppresses TNFα-induced epithelial-mesenchymal transition, cancer cell migration, and invasion. TD1092 is suitable for research on breast cancer, ovarian cancer, melanoma, and inflammation-related diseases^[1]. (Pink: cIAP1 and cIAP2 and XIAP ligand (HY-135997); Blue: Ligands for E3 Ligase ligand (HY-14658); Black: linker).

IC₅₀ & Target

^[1]

cIAP1

cIAP2

XIAP

Caspase 3

Caspase-7

All PROTACs Isoforms :

All IAP Isoforms :

All Caspase Isoforms :

All TNF Receptor Isoforms :

All NF-κB Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	GI₅₀	0.396 μM Compound: 12; TD-1092	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 36410083]

In Vitro

TD1092 (0.1-10 μM; 18 h) potently degrades cIAP1, cIAP2, and XIAP without reducing CRBN levels in MCF-7 cells^[1].
TD1092 (0.1 μM; 0.5-6 h) rapidly degrades the three IAP proteins within 1 hour without affecting CRBN expression in MCF-7 cells^[1].
Degradation of IAP proteins induced by TD1092 in MCF-7 cells is strictly dependent on the functional ubiquitin-proteasome system^[1].
TD1092 (0.01-1 μM; 18 h) concentration-dependently activates caspase 3/7 in MCF-7 cells^[1].
TD1092 (1 μM; 48 h) induces significant levels of apoptotic cell death in MCF-7 cells after 48 h of treatment at 1 μM^[1].
TD1092 (0.1 μM; 2 h pre-treatment followed by 3 min TNFα stimulation) potently inhibits TNFα-induced canonical NF-κB and MAPK signaling pathway activation in MCF-7 cells while increasing RIP1 phosphorylation^[1].
TD1092 (0.1 μM; 24 h) effectively suppresses TNFα-stimulated migration and invasion of MDA-MB-231 triple-negative breast cancer cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

MCF-7 cells
Concentration:

0.1 μM; 1 μM; 10 μM
Incubation Time:

18 h
Result:

Potently degraded cIAP1, cIAP2, and XIAP without reducing CRBN levels.

Western Blot Analysis^[1]

Cell Line:

human breast cancer MCF-7 cells
Concentration:

0.1 μM
Incubation Time:

0.5 h, 1 h, 2 h, 4 h, 6 h
Result:

Induced more than 90% degradation of cIAP1, cIAP2, and XIAP within 1 hour at 0.1 μM.
Maintained unchanged CRBN protein levels across all time points.

Apoptosis Analysis^[1]

Cell Line:

human breast cancer MCF-7 cells
Concentration:

1 μM
Incubation Time:

48 h
Result:

Resulted in 46% of total MCF-7 cells being apoptotic after 48 h of incubation at 1 μM.

Western Blot Analysis^[1]

Cell Line:

human breast cancer MCF-7 cells
Concentration:

0.1 μM
Incubation Time:

2 h (pre-treatment) + 3 min (TNFα stimulation)
Result:

Significantly reduced TNFα-induced phosphorylation of IKK, IκBα, p65, and p38.
Increased phosphorylation of RIP1, suppressing activation of the canonical NF-κB signaling pathway.

Cell Migration Assay ^[1]

Cell Line:

MDA-MB-231 triple-negative breast cancer cells
Concentration:

0.1 μM
Incubation Time:

24 h
Result:

Effectively inhibited the migration and invasion of TNFα-stimulated MDA-MB-231 triple-negative breast cancer cells.

Chemical Information

CAS No. 3037417-26-5
Appearance Solid
분자량 987.19
화학식 C₅₅H₇₀N₈O₉
Color Light yellow to yellow
SMILES

O=C(N[C@@H]1CCCC2=C1C=CC=C2)[C@H]3N(C([C@@H](NC([C@H](C)NC)=O)C(C)(C)C)=O)CC4=C(C=CC(OCCCCCCCCNC(C(C5)CN5C(C=C6C7=O)=CC=C6C(N7C8CCC(NC8=O)=O)=O)=O)=C4)C3
선적

Room temperature in continental US; may vary elsewhere.
보관

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

용액&용해도

In Vitro:

DMSO : ≥ 100 mg/mL (101.30 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0130 mL

5.0649 mL

10.1298 mL

5 mM

0.2026 mL

1.0130 mL

2.0260 mL

10 mM

0.1013 mL

0.5065 mL

1.0130 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Park S, et al. Discovery of pan-IAP degraders via a CRBN recruiting mechanism. European journal of medicinal chemistry. 2023 Jan 05;245(Pt 2):114910. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0130 mL	5.0649 mL	10.1298 mL	25.3244 mL
	5 mM	0.2026 mL	1.0130 mL	2.0260 mL	5.0649 mL
	10 mM	0.1013 mL	0.5065 mL	1.0130 mL	2.5324 mL
	15 mM	0.0675 mL	0.3377 mL	0.6753 mL	1.6883 mL
	20 mM	0.0506 mL	0.2532 mL	0.5065 mL	1.2662 mL
	25 mM	0.0405 mL	0.2026 mL	0.4052 mL	1.0130 mL
	30 mM	0.0338 mL	0.1688 mL	0.3377 mL	0.8441 mL
	40 mM	0.0253 mL	0.1266 mL	0.2532 mL	0.6331 mL
	50 mM	0.0203 mL	0.1013 mL	0.2026 mL	0.5065 mL
	60 mM	0.0169 mL	0.0844 mL	0.1688 mL	0.4221 mL
	80 mM	0.0127 mL	0.0633 mL	0.1266 mL	0.3166 mL
	100 mM	0.0101 mL	0.0506 mL	0.1013 mL	0.2532 mL

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수량:
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TD1092

All PROTACs Isoforms

All IAP Isoforms

All Caspase Isoforms

All TNF Receptor Isoforms

All NF-κB Isoforms